Biochem/physiol Actions

Reversible: yes

Primary TargetG9a and PRC2 HMTases

Cell permeable: yes

General description

A cell-permeable analog of the amino-benzimidazolo BIX-01338 (Cat. No. 539212) and the methylester prodrug of BRD9539 that acts as an SAM-competitive inhibitor against PRC2 and G9a (IC₅₀ ≤6.3 µM) histone methyltransferase activities, displaying little effect toward 10 other HMTases, 9 HDACs, and 100 cellular kinases. Selectively reduces H3K9me2 and H3K9me3 (EC₅₀ = 5 µM) histone methylation levels in pancreatic cancer cells (PANC-1) with much less or little effect toward H3K36me3, H3K4me3, H3K27me3, or H3K6me3 levels. Inhibits both anchorage-dependent and -independent PANC-1 proliferation via ATM activation and G2/M cell-cycle arrest, but not apoptosis induction (no caspase3/7 activation; 10 µM, 72 h).

Legal Information

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

Other Notes

Yuan, Y., et al. 2012. ACS Chem Biol.7, 1152.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)