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5.00580

Sigma-Aldrich

Ezh2 Inhibitor III, GSK126

Synonym(s):

Ezh2 Inhibitor III, GSK126, Enhancer of Zested Homolog 2 Inhibitor III, ( S)-1-( sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1 H-indole-4-carboxamide, HMTase Inhibitor XIV

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About This Item

Empirical Formula (Hill Notation):
C31H38N6O2
Molecular Weight:
526.67
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

form

semisolid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

brown

solubility

DMSO: 10 mg/mL

storage temp.

−20°C

General description

A cell-permeable EI1 (Cat. No. 500561) structural analog that acts as an equally potent, SAM-competitive, Ezh2/PRC2 inhibitor (Ki = 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2; [SAM] = 7.5 µM) with similar selectivity over Ezh1/PRC2 (Ki = 89 nM) and other HTMases as EI1. Among panels of 14 HDACs, 11 GPCRs, and 300 kinases, only serotonin 3 receptor, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50 ≥4 µM). Shown to inhibit the proliferation of DLBCL (IC50 28 nM to 5.5 µM; 6 d treatment) in vitro and completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo (50 mg/kg/d i.p.). In addition to DLBCL (diffuse large B cell lymphoma; IC50 ranges from 28 nM to 5.5 µM; 6 d treatment), GSK126 is also shown to inhibit the proliferation of other B-NHL (non-Hodgkin′s lymphoma) and Hodgkin′s lymphoma cell lines, being least active against MC116, HD-MY-Z, WSU-FSCCL, Toledo, NU-DUL-1, and WILL-2 (IC50 >10 µM; 6 d treatment). When administered at a daily i.p. dose of 50 mg/kg, GSK126 is reported to completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo, while complete tumor eradication can be achieved with higher dosing regimens (150 mg/kg/day or two 300 mg/kg dosages per week). It has been demonstrated to regulate the EZH2-PAX6-CXCL10 pathway, thereby suppressing myocardial fibrosis. Additionally, GSK126 has been observed to inhibit apoptosis and reduce H3K27me3 levels in the brains of rat models.

Application

GSK126, Ezh2 Inhibitor III has been used:
  • in testing the epigenetic interactions for the formation of single-cell domains.
  • to induce hyper histone methylation in IMR-90 cells.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.

Other Notes

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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