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> JQ1 (+) [1268524-70-4]

JQ1 (+) [1268524-70-4]

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JQ1 (+) [1268524-70-4]

JQ1 (+) | BET Bromodomain inhibitor

CAS:
1268524-70-4
Catalog Number:
10-1584
Activity:
BET Bromodomain inhibitor
Chemical Name:
(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Molecular Weight:
456.99
Molecular Formula:
C23H25ClN4O2S
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

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5 mg$100.00
25 mg$400.00
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JQ1 (+) (1268524-70-4) is a potent BET bromodomain inhibitor and is the active isomer.   IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer).1 Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models.1 Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts.2 Displays reversible contraceptive effects in male mice.3 Blocks inflammation and bone loss in periodontitis.4 Reverses CAR T cell extinction.5

References/Citations:

  1. Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067
  2. Herrmann et al. (2012), Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML; Oncotarget, 3 1588
  3. Matzuk et al. (2012), Small-molecule inhibition of BRDT for male contraception; Cell 150 673
  4. Meng et al. (2014), BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction;, J. Dent. Res. 93 657
  5. Kong et al. (2021), BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia; J. Clin. Invest., 131 e145459
CAS:
1268524-70-4
Catalog Number:
10-1584
Activity:
BET Bromodomain inhibitor
Chemical Name:
(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Molecular Weight:
456.99
Molecular Formula:
C23H25ClN4O2S
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Download Product Data Sheet

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a restocking/refund fee

JQ1 (+) (1268524-70-4) is a potent BET bromodomain inhibitor and is the active isomer.   IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer).1 Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models.1 Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts.2 Displays reversible contraceptive effects in male mice.3 Blocks inflammation and bone loss in periodontitis.4 Reverses CAR T cell extinction.5

References/Citations:

  1. Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067
  2. Herrmann et al. (2012), Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML; Oncotarget, 3 1588
  3. Matzuk et al. (2012), Small-molecule inhibition of BRDT for male contraception; Cell 150 673
  4. Meng et al. (2014), BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction;, J. Dent. Res. 93 657
  5. Kong et al. (2021), BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia; J. Clin. Invest., 131 e145459