HY-10224-10mg | Panobinostat [404950-80-7] Clinisciences

Beschreibung

Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities^[1]^[2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells^[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma^[3].

IC₅₀ & Target^[1]^[5]

HDAC

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.035 μM Compound: LBH589	Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
A2780	EC₅₀	150.71 nM Compound: LBH-589	Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay	[PMID: 27186676]
A2780	EC₅₀	169.5 nM Compound: LBH-589	Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay	[PMID: 27186676]
A2780	IC₅₀	54.8 nM Compound: Panobinostat	Antiproliferative activity against human A2780 cells after 72 hrs by microplate reader based MTT assay Antiproliferative activity against human A2780 cells after 72 hrs by microplate reader based MTT assay	[PMID: 31431326]
A2780	IC₅₀	7.67 nM Compound: Panobinostat	Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay	[PMID: 31431326]
A2780	IC₅₀	8.32 nM Compound: LBH-589	Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 27186676]
A549	IC₅₀	0.02 μM Compound: Panobinostat	Antiproliferative activity against human A549 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells measured after 72 hrs by CCK8 assay	[PMID: 31272794]
B16	GI₅₀	0.15 μM Compound: LBH589	Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay	[PMID: 23009203]
Bel-7402	IC₅₀	21.28 nM Compound: LBH589	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human Bel7402 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
CAL-148	IC₅₀	< 0.1 μM Compound: Panobinostat	Antiproliferative activity against human CAL148 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human CAL148 cells measured after 72 hrs by CCK8 assay	[PMID: 31272794]
CAL-27	IC₅₀	10.9 nM Compound: Panobinostat	Antiproliferative activity against human CAL27 cells after 72 hrs by microplate reader based MTT assay Antiproliferative activity against human CAL27 cells after 72 hrs by microplate reader based MTT assay	[PMID: 31431326]
COLO 205	IC₅₀	0.018 μM Compound: LBH589	Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
EBC-1	IC₅₀	27.85 nM Compound: LBH589	Antiproliferative activity against human EBC1 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human EBC1 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
HCT-116	IC₅₀	0.048 μM Compound: LBH589	Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	IC₅₀	3.36 nM Compound: LBH-589	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 27186676]
HEK293	CC₅₀	0.028 μM Compound: Panobinostat	Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 30973727]
HEK293	IC₅₀	0.07 μM Compound: 34	Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay	[PMID: 28241112]
HEK293	IC₅₀	11 nM Compound: LBH589	Inhibition of HDAC6 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of HDAC6 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
HEK293	IC₅₀	2.1 nM Compound: LBH589	Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
HEK293	IC₅₀	2.5 nM Compound: LBH589	Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
HEK293	IC₅₀	200 nM Compound: LBH589	Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
HEK293	IC₅₀	70 nM Compound: Panobinostat	Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay	[PMID: 30245402]
HeLa	IC₅₀	0.83 nM Compound: LBH-589	Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay	[PMID: 27186676]
HeLa	IC₅₀	22 nM Compound: LBH589	Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay	[PMID: 31400937]
HeLa	IC₅₀	30 nM Compound: LBH589	Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay	[PMID: 23639537]
HepG2	CC₅₀	< 0.078 μM Compound: Panobinostat	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay	[PMID: 30973727]
HepG2	IC₅₀	< 0.1 μM Compound: Panobinostat	Antiproliferative activity against human HepG2 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells measured after 72 hrs by CCK8 assay	[PMID: 31272794]
HT-29	IC₅₀	37.55 nM Compound: LBH589	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
Huh-7	CC₅₀	0.0035 μM Compound: 8, LBH589	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay	[PMID: 25490700]
HuT78	EC₅₀	4.3 nM Compound: 2	Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay	[PMID: 30122227]
KM3/BTZ	IC₅₀	150 nM Compound: LBH-589	Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay	[PMID: 32267687]
KM3/BTZ	IC₅₀	20.1 nM Compound: LBH-589	Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay	[PMID: 32267687]
MCF7	IC₅₀	9 nM Compound: LBH589	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
MDA-MB-231	IC₅₀	29.13 nM Compound: LBH589	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
MM1.S	GI₅₀	8.9 nM Compound: 2	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay	[PMID: 33661013]
MV4-11	EC₅₀	< 30 nM Compound: Panobinostat	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay	[PMID: 27754681]
MV4-11	IC₅₀	2.97 nM Compound: LBH-589	Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 27186676]
MV4-11	EC₅₀	5.2 nM Compound: Pan; LBH589	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis	[PMID: 32321249]
NCI-H1975	IC₅₀	17.51 nM Compound: LBH589	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
NCI-N87	IC₅₀	8.42 nM Compound: LBH589	Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]
NFF	IC₅₀	0.07 μM Compound: 34	Cytotoxicity against human NFF cells after 72 hrs by SRB assay Cytotoxicity against human NFF cells after 72 hrs by SRB assay	[PMID: 28241112]
NFF	IC₅₀	70 nM Compound: Panobinostat	Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay	[PMID: 30245402]
PANC-1	IC₅₀	1 μM Compound: Panobinostat	Cytotoxicity against human PANC1 cells assessed as reduction in cell viability incubated upto 72 hrs by MTT assay Cytotoxicity against human PANC1 cells assessed as reduction in cell viability incubated upto 72 hrs by MTT assay	[PMID: 33951490]
PC-3	IC₅₀	0.024 μM Compound: LBH589	Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
Sf21	IC₅₀	13 nM Compound: LBH589	Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
Sf9	IC₅₀	> 10000 nM Compound: LBH-589	Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay	[PMID: 27186676]
Sf9	IC₅₀	> 10000 nM Compound: LBH-589	Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay	[PMID: 27186676]
Sf9	IC₅₀	> 20000 nM Compound: LBH589	Inhibition of recombinant N-terminal GST-tagged full length human HDAC5 expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay Inhibition of recombinant N-terminal GST-tagged full length human HDAC5 expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay	[PMID: 31855601]
Sf9	IC₅₀	> 20000 nM Compound: LBH589	Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as susbtrate after 24 hrs by fluorescence based assay Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as susbtrate after 24 hrs by fluorescence based assay	[PMID: 31855601]
Sf9	IC₅₀	> 20000 nM Compound: LBH589	Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay	[PMID: 31855601]
Sf9	IC₅₀	0.001 μM Compound: LBH-589	Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate	[PMID: 27377864]
Sf9	IC₅₀	0.002 μM Compound: LBH-589	Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay	[PMID: 27377864]
Sf9	IC₅₀	0.002 μM Compound: LBH-589	Inhibition of human recombinant HDAC6 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay Inhibition of human recombinant HDAC6 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay	[PMID: 27377864]
Sf9	IC₅₀	0.092 μM Compound: LBH-589	Inhibition of N-terminal GST-tagged full length human recombinant HDAC5 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen Inhibition of N-terminal GST-tagged full length human recombinant HDAC5 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen	[PMID: 27377864]
Sf9	IC₅₀	0.231 μM Compound: LBH-589	Inhibition of C-terminal His-tagged full length human recombinant HDAC8 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen Inhibition of C-terminal His-tagged full length human recombinant HDAC8 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen	[PMID: 27377864]
Sf9	IC₅₀	0.373 μM Compound: LBH-589	Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as	[PMID: 27377864]
Sf9	IC₅₀	1.26 nM Compound: LBH-589	Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a	[PMID: 27186676]
Sf9	IC₅₀	1.673 nM Compound: Pan; LBH589	Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins	[PMID: 32321249]
Sf9	IC₅₀	1.926 nM Compound: Pan; LBH589	Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins	[PMID: 32321249]
Sf9	IC₅₀	190.3 nM Compound: LBH-589	Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay	[PMID: 27186676]
Sf9	IC₅₀	2.059 nM Compound: Pan; LBH589	Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins	[PMID: 32321249]
Sf9	IC₅₀	2.097 nM Compound: Pan; LBH589	Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins	[PMID: 32321249]
Sf9	IC₅₀	2.1 nM Compound: Pan; LBH589	Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr fo Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr fo	[PMID: 32321249]
Sf9	IC₅₀	2.27 nM Compound: LBH-589	Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr	[PMID: 27186676]
Sf9	IC₅₀	2.68 μM Compound: LBH-589	Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by	[PMID: 27377864]
Sf9	IC₅₀	2.83 μM Compound: LBH-589	Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by	[PMID: 27377864]
Sf9	IC₅₀	280 nM Compound: LBH589	Inhibition of his-strep-tagged HDAC8 (unknown origin) expressed in SF9 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting Inhibition of his-strep-tagged HDAC8 (unknown origin) expressed in SF9 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting	[PMID: 22344701]
Sf9	IC₅₀	3.28 nM Compound: LBH-589	Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a	[PMID: 27186676]
Sf9	IC₅₀	337.8 nM Compound: LBH-589	Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat	[PMID: 27186676]
Sf9	IC₅₀	4.16 nM Compound: LBH-589	Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a	[PMID: 27186676]
Sf9	IC₅₀	4.45 nM Compound: LBH-589	Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay	[PMID: 27186676]
Sf9	IC₅₀	4.86 nM Compound: LBH-589	Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after	[PMID: 27186676]
Sf9	IC₅₀	4112 nM Compound: LBH-589	Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence	[PMID: 27186676]
Sf9	IC₅₀	4354 nM Compound: LBH-589	Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu	[PMID: 27186676]
Sf9	IC₅₀	887.8 nM Compound: LBH-589	Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas	[PMID: 27186676]
T47D	IC₅₀	6.98 nM Compound: LBH589	Antiproliferative activity against human T47D cells assessed as reduction in cell growth after 72 hrs Antiproliferative activity against human T47D cells assessed as reduction in cell growth after 72 hrs	[PMID: 31855601]

In Vitro

Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells^[1]. Panobinostat exhibites potent antiproliferative activity in human NSCLC cell lines with the IC₅₀ ranging from 5 to 100 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice^[2]. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Klinische Studie

Molekulargewicht

349.43

Formel

C₂₁H₂₃N₃O₂

CAS. Nr.

404950-80-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(/C=C/C1=CC=C(CNCCC2=C(NC3=C2C=CC=C3)C)C=C1)NO

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (286.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8618 mL	14.3090 mL	28.6180 mL
5 mM	0.5724 mL	2.8618 mL	5.7236 mL
10 mM	0.2862 mL	1.4309 mL	2.8618 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner
Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.15 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.37%

Select Batch:

SDS (805 KB)

COA (250 KB) LCMS (107 KB) Elemental Analysis Report (108 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100. [Content Brief]

[2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31. [Content Brief]

[3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803. [Content Brief]

[4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147. [Content Brief]

[5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8. [Content Brief]

Zellassay ^[1]	Cells are washed with ice-cold PBS containing 0.1 mM sodium orthovanadate, and total proteins are isolated using RIPA lysis buffer, which includes protease inhibitors (leupeptin, antipain, and aprotinin), 0.5 mM PMSF, and 0.2 mM sodium orthovanadate. Protein amounts are quantified using the Bio-Rad protein assay. Equal amounts of proteins are loaded onto an sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) gel, transferred onto nitrocellulose membrane, and probed with the antibody of interest: mouse monoclonal c-Myc and mouse monoclonal p21 antibodies; rabbit polyclonal phospho-Histone H2A.X, rabbit polyclonal acetyl-Histone H3 (Lys9), and rabbit polyclonal acetyl-Histone H4 (Lys8) antibodies; mouse monoclonal p27/KIP1 antibody; mouse monoclonal anti-β-actin; and mouse monoclonal anti-GADD45G. Membranes are then washed, reprobed with appropriate horseradish peroxidase-conjugated secondary antibodies, and developed with SuperSignal chemiluminescent substrate. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[1]	AE17 and TC-1 cancer cells (1×10⁶ cells) are injected into the flanks of adult female C57Bl/6 mice and severe combined immunodeficiency (SCID) mice. M30 (10×10⁶ cells), A549 (5×10⁶ cells), H69 (2.5×10⁶ cells), BK-T (6.5×10⁶), H526 (10×10⁶), and RG1 (10×10⁶) cells are also injected, but in the presence of matrigel, into the flanks of SCID mice. When tumors reach 100 to 500 mm³, panobinostat is administered via i.p. injections (10-20 mg/kg) on a daily schedule (5-days-on, 2-days-off regimen) for the entire duration of the experiment. Control micereceive i.p. injections with dextrose 5% in water. Every tumor is measured with a caliper at least twice weekly. For evaluation of the effects of combination therapy on SCLC-derived tumors, SCID mice with H69 tumors are administered panobinostat. Three days after the initiation of panobinostat, and again 1 wk later, etoposide (40 mg/kg) is administered i.p. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise	[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100. [Content Brief] [2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31. [Content Brief] [3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803. [Content Brief] [4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147. [Content Brief] [5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8618 mL	14.3090 mL	28.6180 mL	71.5451 mL
	5 mM	0.5724 mL	2.8618 mL	5.7236 mL	14.3090 mL
	10 mM	0.2862 mL	1.4309 mL	2.8618 mL	7.1545 mL
	15 mM	0.1908 mL	0.9539 mL	1.9079 mL	4.7697 mL
	20 mM	0.1431 mL	0.7155 mL	1.4309 mL	3.5773 mL
	25 mM	0.1145 mL	0.5724 mL	1.1447 mL	2.8618 mL
	30 mM	0.0954 mL	0.4770 mL	0.9539 mL	2.3848 mL
	40 mM	0.0715 mL	0.3577 mL	0.7155 mL	1.7886 mL
	50 mM	0.0572 mL	0.2862 mL	0.5724 mL	1.4309 mL
	60 mM	0.0477 mL	0.2385 mL	0.4770 mL	1.1924 mL
	80 mM	0.0358 mL	0.1789 mL	0.3577 mL	0.8943 mL
	100 mM	0.0286 mL	0.1431 mL	0.2862 mL	0.7155 mL

Panobinostat Related Classifications

Cell Cycle/DNA Damage Epigenetics Autophagy Anti-infection Apoptosis
HDAC Autophagy HIV Apoptosis

Panobinostat [404950-80-7]

Katalog-Nummer HY-10224-10mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of Panobinostat:

Alle HDAC Isoform-spezifische Produkte anzeigen:

Alle HIV Isoform-spezifische Produkte anzeigen:

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Panobinostat Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein:

Panobinostat [404950-80-7]

Katalog-Nummer HY-10224-10mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of Panobinostat:

Alle HDAC Isoform-spezifische Produkte anzeigen:

Alle HIV Isoform-spezifische Produkte anzeigen:

Panobinostat Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Panobinostat Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein: