Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

MG-132 [133407-82-6]

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Referentie HY-13259-5mg

Formaat : 5mg

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MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC₅₀s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.

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MG-132 Chemical Structure

CAS No. : 133407-82-6

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Based on 1135 publication(s) in Google Scholar

Other Forms of MG-132:

(R)-MG-132 Obtenir un devis
MG-132 (negative control) Obtenir un devis

: MG-132 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb 20;189:106704. [Abstract]; MG132 (10 µM) significantly reduces the degradation of YTHDC1 protein mediated by Dihydroartemisinin (DHA) in HSCs.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2023 Feb 13;307:116243. [Abstract]; Both MG-132 (10 μM) and Baf A1 (10 μM) markedly increase TGF-β1 protein expression in HG-stimulated SV40-MES-13 cells (Fig. C and D).

: MG-132 purchased from MedChemExpress. Usage Cited in: J Virol. 2023 Mar 6;e0198422. [Abstract]; MG-132 (200 nM; 24 h) significantly inhibits Newcastle disease virus (NDV) infection-caused degradation of β-catenin in DF-1 cells.

: MG-132 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107990. [Abstract]; PMs are treated with MG132 (10 μM). Endogenous YAP protein accumulated in the presence of MG132 starts from 2 h and further increases at 4 and 6 h after treatment in WT macrophages.

: MG-132 purchased from MedChemExpress. Usage Cited in: Brain Behav Immun. 2019 Jul;79:244-255. [Abstract]; Effect of autolysosome inhibitor (chloroquine, CQ, 50 μM) or proteasome inhibitor (MG132, 5 μM) on KA-induced NLRP3 degradation. Cells are treated with the inhibitors for 0.5 h before KA (10 μM, 2 h) treatment.

: MG-132 purchased from MedChemExpress. Usage Cited in: EMBO J. 2019 Mar 15;38(6):e100376. [Abstract]; Brcc3^+/+ and Brcc3^-/- (Abro1^+/+ and Abro1^-/-)BMDMs are treated with or without LPS for 1 h. Before LPS treatment, Brcc3^-/- (Abro1^-/-) BMDMs are pretreated with MG132 (10 μM) for 6 h to rescue the expression of ABRO1. Immunoblot analysis of NLRP3 and ABRO1 proteins in cell lysates immunoprecipitated with anti-ABRO1 antibody.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 26;38(1):101. [Abstract]; HLF and Hep3B cells are treated with Mg132 (10 μg/ml) for 4 h, total protein is extracted and subjected to western blotting using anti-Flag, anti-p21, or anti-GAPDH antibodies.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Exp Bot. 2019 Sep 24;70(18):4749-4762. [Abstract]; Cell-free degradation assay of recombinant His-PhCHS protein. Recombinant His- PhCHS is purified from Escherichia coli incubated with petal crude proteins at stages and treated with specific 26S proteasome inhibitor MG132 at various time intervals. Western blot analysis was conducted using an anti-His antibody and anti-β-actin protein concentration was used as a loading control.

: MG-132 purchased from MedChemExpress. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848. [Abstract]; Tan-IIA increases the endogenous induction of Nrf2 induction and this effect is further enhanced by cotreatment with the proteasome inhibitor MG-132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Molecules. 2019 Jan 22;24(3):393. [Abstract]; The HepG2 cells are pretreated for 5 h MG 132 which is a proteasome inhibitor. Then, the MARCH1 protein expressions in HepG2 cells treated with 0 μM, 5,0 μM SAF, and 2.5 μM MG 132 are measured by immunoblotting.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 3;37(1):240. [Abstract]; Decrease of ERCC6 expression can be rescued with proteasome inhibitor MG132. Subconfluent SKOV3 cells are treated with FL118 and MG132 alone or in combination as shown for 8 h, followed by western blot analyses with ERCC6 antibody.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 15;37(1):193. [Abstract]; Western blot is performed in HCC-LM3 cells transfected with HJURP knockdown lentivirus and treated with DMSO or MG132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2019 Feb 1;79(3):534-545. [Abstract]; Cells are transfected with GYS2 siRNA and pre-incubated with MG-132 (20 μM) for 12 h. Cell lysate are immunoprecipitated by anti-Ub and immunoblotted by anti-p53.

: MG-132 purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2018 Aug;34:243-255. [Abstract]; MPC1 protein expression in primary mouse hepatocytes incubated with pyruvate for 8 h in the presence of MG-132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604. [Abstract]; Different concentrations of two classical proteasome inhibitors PS-341 and MG132 are added. AGS cells are either untreated or treated with PS-341 (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

: MG-132 purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2018 Aug;51(4):e12451. [Abstract]; Immunoblot analysis of CDK4 in cells treated with 4 μM of CGN for 24 hours in the presence and absence of MG132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Feb 1;146:251-259. [Abstract]; In the absence of MG132, the protein degradation pathways are intact, the Tau protein level is significantly decreased in peptide 1-treated group.

: MG-132 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523. [Abstract]; The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

: MG-132 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Apr 19;9:377. [Abstract]; Immunoblot levels of highly molecular weight (HMW)-ubiquitinated proteins and pSer129-α-syn after inhibiting the ubiquitin-proteasome system (UPS) by various concentrations of MG132 (0.25, 0.5, and 1 μM) in SH-SY5Y cells.

: MG-132 purchased from MedChemExpress. Usage Cited in: Mol Plant Pathol. 2018 Dec;19(12):2623-2634. [Abstract]; Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2018;17(13):1591-1601. [Abstract]; The protein level of CCNB1 in different groups is analyzed by Western blot; MG132 significantly increases the protein level of CCNB1 in oocytes from CRS group mice. Western blotting showing the reduced expression of securin is rescued by MG132 in CRS group mouse oocytes.

: MG-132 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78. [Abstract]; Western analysis of proteins expression with treatment of IKK-16 or MG-132.

: MG-132 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Nov;16(5):5900-5906. [Abstract]; Treatment with the 26S proteasome inhibitor, MG 132 (10 µM), rescues the downregulation of NEK 8 in the pVHL overexpressing SGC 7901 cells.

: MG-132 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338. [Abstract]; The neonatal rat cardiomyocytes (NRCMs) are treated with MG132 (10 μM). The protein expression level of PPARα in the indicated group.

: MG-132 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Dec 1;410:112-123. [Abstract]; Immunoprecipitation of ubiquitin from lysates of U-2 OS cells expressing CHOP after treatment with different concentrations of MG7 for 48 h. Cells are incubated with MG132 (20 mM) for 4 h before harvest. Cell lysates are immunoblotted with the indicated antibodies.

: MG-132 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929. [Abstract]; p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80 μM ω-3 FFAs, 20 μM ATRA alone or in combination for 48 h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

: MG-132 purchased from MedChemExpress. Usage Cited in: J Inorg Biochem. 2017 Oct;175:92-100. [Abstract]; TPEN-triggered PML-RARα degradation in NB4 cells is reversed by MG-132 treatment. NB4 cells are treated with 5 μM TPEN with or without the presence of 1 μM MG-132 for the indicated durations (0–12 h) and then lysed. The lysates are analyzed for PML-RARα and RARα protein levels by western blotting.

: MG-132 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Sep 2;490(4):1168-1175. [Abstract]; Treatment of CHO-K1 cells with proteasome inhibitor, MG-132 results in elevated SR-B1 protein levels. The cells with MG-132, a potent proteasome inhibitor that inhibit ubiquitin/proteasome-dependent protein degradation, and MG-132 treatment significantly enhances cellular SR-B1 protein level.

: MG-132 purchased from MedChemExpress. Usage Cited in: Université de Montréal. Octobre 2017.; Unsynchronized control and ARF6 cells are treated with DMSO or MG132 (10 μM) for 1h or 4h, lysed and total ubiquitinated proteins are determined using western blot (n=3).

Description

IC₅₀ & Target

IC50: 100 nM (Proteasome), 1.2 μM (Calpain)^[1]^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	< 10 μM Compound: MG132	Cytotoxicity against african green monkey COS7 cells by XTT method Cytotoxicity against african green monkey COS7 cells by XTT method	[PMID: 18088097]
HCT-116	IC₅₀	0.82 μM Compound: MG132	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31312413]
HEK293	IC₅₀	0.009 μM Compound: MG132	Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay	[PMID: 23540790]
HEK293	IC₅₀	0.6 μM Compound: MG132	Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay	[PMID: 23540790]
Huh-7	IC₅₀	< 10 μM Compound: MG132	Cytotoxicity against human HuH7 cells by XTT method Cytotoxicity against human HuH7 cells by XTT method	[PMID: 18088097]
MCF-10A	IC₅₀	0.29 μM Compound: MG-132	Growth inhibition of human MCF10A cells after 72 hrs by CellTiter-Blue assay Growth inhibition of human MCF10A cells after 72 hrs by CellTiter-Blue assay	[PMID: 24153206]
MCF7	IC₅₀	0.13 μM Compound: MG-132	Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay	[PMID: 24153206]
MDA-MB-231	IC₅₀	0.18 μM Compound: MG-132	Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay	[PMID: 24153206]
NCI-H23	IC₅₀	0.48 μM Compound: MG-132	Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H727	IC₅₀	0.98 μM Compound: MG-132	Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H929	IC₅₀	0.17 μM Compound: MG-132	Cytotoxicity against human NCI-H929 cells after 3 days by Alamar blue assay Cytotoxicity against human NCI-H929 cells after 3 days by Alamar blue assay	[PMID: 24625088]
OCI-Ly3	IC₅₀	> 10 μM Compound: 1, MG-132	Cytotoxicity against NF-kappaB overexpressing human OCI-Ly3 cells after 4 hrs Cytotoxicity against NF-kappaB overexpressing human OCI-Ly3 cells after 4 hrs	[PMID: 18024113]
RAW264.7	IC₅₀	0.08 μg/mL Compound: MG132	Inhibition of LPS and IFN-gamma-stimulated nitric oxide production in mouse RAW264.7 cells after 18 hrs by Griess method Inhibition of LPS and IFN-gamma-stimulated nitric oxide production in mouse RAW264.7 cells after 18 hrs by Griess method	[PMID: 26351042]
RAW264.7	IC₅₀	0.08 μM Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent method	[PMID: 22620677]
RAW264.7	IC₅₀	0.1 μM Compound: MG132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 18 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 18 hrs by Griess method	[PMID: 33422907]
RAW264.7	IC₅₀	0.1 μM Compound: MG-132	Inhibition of LPS-stimulated NO production in mouse RAW264.7 cells after 18 hrs by Griess assay Inhibition of LPS-stimulated NO production in mouse RAW264.7 cells after 18 hrs by Griess assay	[PMID: 24219809]
RAW264.7	IC₅₀	0.1 μM Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method	[PMID: 23819871]
RAW264.7	IC₅₀	0.1 μM Compound: MG132	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells by Griess method Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells by Griess method	[PMID: 24597894]
RAW264.7	IC₅₀	0.1 μM Compound: MG-132	Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 18 hrs by griess reagent based plate reader analysis Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 18 hrs by griess reagent based plate reader analysis	[PMID: 24697496]
RAW264.7	IC₅₀	0.15 μM Compound: MG-132	Inhibition of LPS-induced NO production in mouse RAW264.7 cells at 25 uM preincubated with compound followed by LPS challenge measured after 18 hrs by Griess method Inhibition of LPS-induced NO production in mouse RAW264.7 cells at 25 uM preincubated with compound followed by LPS challenge measured after 18 hrs by Griess method	[PMID: 26757019]
RAW264.7	IC₅₀	0.15 μM Compound: MG-132	Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells measured after 18 hrs by Griess reagent based multilabel plate reader analysis Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells measured after 18 hrs by Griess reagent based multilabel plate reader analysis	[PMID: 23327668]
RAW264.7	IC₅₀	0.16 μM Compound: MG-132	Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent based assay Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent based assay	[PMID: 30629435]
RAW264.7	IC₅₀	0.17 μg/mL Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 5 mins by Greiss method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 5 mins by Greiss method	[PMID: 22277277]
RAW264.7	IC₅₀	0.17 μg/mL Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-induced NO production after 5 mins by Greiss method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-induced NO production after 5 mins by Greiss method	[PMID: 22277277]
RAW264.7	IC₅₀	0.18 μM Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess assay	[PMID: 27203291]
RAW264.7	IC₅₀	0.2 μM Compound: MG132	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated iNOS activity preincubated with compound for 24 hrs followed by LPS stimulation for 2 hrs and measured 2 hrs after NADPH addition by fluorescence based assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated iNOS activity preincubated with compound for 24 hrs followed by LPS stimulation for 2 hrs and measured 2 hrs after NADPH addition by fluorescence based assay	[PMID: 33454546]
RAW264.7	IC₅₀	0.2 μM Compound: MG132	Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells preincubated with compound for 24 hrs followed by LPS stimulation and measured after 2 hrs by Griess reagent-based assay Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells preincubated with compound for 24 hrs followed by LPS stimulation and measured after 2 hrs by Griess reagent-based assay	[PMID: 33454546]
RAW264.7	IC₅₀	0.2 μM Compound: MG-132	Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production preincubated for 1 hr followed by LPS stimulation measured after 18 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production preincubated for 1 hr followed by LPS stimulation measured after 18 hrs by Griess assay	[PMID: 29338260]
RAW264.7	IC₅₀	0.35 μM Compound: MG-132	Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 18 hrs Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 18 hrs	[PMID: 21044847]
RAW264.7	IC₅₀	0.35 μM Compound: MG-132	Inhibition of NO production in Interferon gamma-stimulated mouse RAW264.7 cells after 18 hrs Inhibition of NO production in Interferon gamma-stimulated mouse RAW264.7 cells after 18 hrs	[PMID: 21044847]
RAW264.7	IC₅₀	0.63 μM Compound: MG132	Toxicity against mouse RAW264.7 cells by XTT assay Toxicity against mouse RAW264.7 cells by XTT assay	[PMID: 22858297]
RAW264.7	IC₅₀	2.6 μM Compound: MG132	Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated with compound for 2 hrs followed by LPS stimulation for 12 hrs by Griess reagent based analysis Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated with compound for 2 hrs followed by LPS stimulation for 12 hrs by Griess reagent based analysis	[PMID: 36607819]
SW480	IC₅₀	29.5 μM Compound: MG132	Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay	[PMID: 26841168]

In Vitro

MG-132 (Z-Leu-Leu-Leu-al) initiates neurite outgrowth in PC12 cells at a low concentration (30 nM) and is a very strong inhibitor of 20S proteasome^[3].
MG-132 (10 μM; 1 hour) reverses the effects of TNF- α on I κ B degradation and NF-κ B activation in A549 cells^[4].
MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition^[5].
MG-132 (10-40 μM; 24 hours) significantly reduces the viability of C6 glioma cells in both time- and concentration-dependent manners and shows the IC₅₀ of 18.5 μM at 24 hours^[6].
MG-132 (18.5 μM; 24 hours) induces down-regulation of anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3^[6].

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

Cell Viability Assay^[3]

Cell Line:	C6 glioma cells
Concentration:	10, 20, 30, 40 μM
Incubation Time:	24 hours
Result:	Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC₅₀ of 18.5 μM at 24 hours.

Western Blot Analysis^[3]

Cell Line:	A549 cells
Concentration:	10 μM
Incubation Time:	1 hour
Result:	Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.

In Vivo

MG132 (10 mg/kg; i.p.; daily for 25 days starting 5 days after EC9706 cells injection) significantly inhibits tumor growth of the EC9706 xenograft without causing toxicity to mice^[7].
MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors^[8].
MG-132 (1-10 μg/kg/24 hours; subcutaneously implanted osmotic pumps; for 8 days) greatly increases the expression levels of β-dystroglycan, α-dystroglycan, α-sarcoglycan, and dystrophin in skeletal muscle lysates in mice (six-month-old male C57BL/10ScSn DMD mdx mice)^[9].

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

Animal Model:	5- to 6-weeks old female athymic nude mice (EC9706 xenograft)
Dosage:	10 mg/kg
Administration:	I.p.; daily for 25 days starting 5 days after EC9706 cells injection
Result:	Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.

Animal Model:	Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells)^[8]
Dosage:	1 mg/kg
Administration:	Intravenous injection; twice a week for 4 weeks
Result:	The growth inhibition rates in HeLa tumors was 49% compared to the control.

Masse moléculaire

475.62

Formule

C₂₆H₄₁N₃O₅

CAS No.

133407-82-6

Appearance

Solid

Color

White to yellow

SMILES

O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C(18)=O)CC(C)C)=O)=O)CC(C)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (210.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1025 mL	10.5126 mL	21.0252 mL
5 mM	0.4205 mL	2.1025 mL	4.2050 mL
10 mM	0.2103 mL	1.0513 mL	2.1025 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité
Calculateur de dilution

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: ≥ 1.67 mg/mL (3.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 1.67 mg/mL (3.51 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Pureté et documentation

Purity: 99.97%

Select Batch:

SDS (393 KB)

COA (246 KB) HNMR (280 KB) RP-HPLC (215 KB) MS (69 KB) Elemental Analysis Report (104 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313. [Content Brief]

[2]. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25. [Content Brief]

[3]. Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6. [Content Brief]

[4]. Fiedler MA, et al. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132. Am J Respir Cell Mol Biol. 1998 Aug;19(2):259-68. [Content Brief]

[5]. MacLaren AP, et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001 Mar;8(3):210-8. [Content Brief]

[6]. Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 2009 Jul;22(1):215-21. [Content Brief]

[7]. Dang L, et al. Proteasome inhibitor MG132 inhibits the proliferation and promotes the cisplatin-inducedapoptosis of human esophageal squamous cell carcinoma cells. Int J Mol Med. 2014 May;33(5):1083-8. [Content Brief]

[8]. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81. [Content Brief]

[9]. Bonuccelli G, et al. Proteasome inhibitor (MG-132) treatment of mdx mice rescues the expression and membrane localization of dystrophin and dystrophin-associated proteins. Am J Pathol. 2003 Oct;163(4):1663-75. [Content Brief]

[1]. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313.

[2]. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May;32(5):619-25.

[3]. Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6.

[4]. Fiedler MA, et al. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132. Am J Respir Cell Mol Biol. 1998 Aug;19(2):259-68.

[5]. MacLaren AP, et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001 Mar;8(3):210-8.

[6]. Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 2009 Jul;22(1):215-21.

[7]. Dang L, et al. Proteasome inhibitor MG132 inhibits the proliferation and promotes the cisplatin-inducedapoptosis of human esophageal squamous cell carcinoma cells. Int J Mol Med. 2014 May;33(5):1083-8.

[8]. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81.

[9]. Bonuccelli G, et al. Proteasome inhibitor (MG-132) treatment of mdx mice rescues the expression and membrane localization of dystrophin and dystrophin-associated proteins. Am J Pathol. 2003 Oct;163(4):1663-75.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1025 mL	10.5126 mL	21.0252 mL	52.5630 mL
	5 mM	0.4205 mL	2.1025 mL	4.2050 mL	10.5126 mL
	10 mM	0.2103 mL	1.0513 mL	2.1025 mL	5.2563 mL
	15 mM	0.1402 mL	0.7008 mL	1.4017 mL	3.5042 mL
	20 mM	0.1051 mL	0.5256 mL	1.0513 mL	2.6281 mL
	25 mM	0.0841 mL	0.4205 mL	0.8410 mL	2.1025 mL
	30 mM	0.0701 mL	0.3504 mL	0.7008 mL	1.7521 mL
	40 mM	0.0526 mL	0.2628 mL	0.5256 mL	1.3141 mL
	50 mM	0.0421 mL	0.2103 mL	0.4205 mL	1.0513 mL
	60 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8760 mL
	80 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6570 mL
	100 mM	0.0210 mL	0.1051 mL	0.2103 mL	0.5256 mL

MG-132 Related Classifications

Metabolic Enzyme/Protease Autophagy Apoptosis
Proteasome Autophagy Apoptosis

MG-132 [133407-82-6]

Referentie HY-13259-5mg

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Merk : MedChemExpress

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Other Forms of MG-132:

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MG-132 Related Classifications

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MG-132 [133407-82-6]

Referentie HY-13259-5mg

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of MG-132:

MG-132 Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

MG-132 Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten: