Key Specifications Table
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|382194-10MG||Glass bottle||10 mg||
|Overview||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).|
|Synonyms||Methyl-2-benzamido-1-(3-phenylpropyl)-1H-benzo[d]imidazole-5-carboxylate, EHMT2/G9a Inhibitor VI|
|References||Yuan, Y., et al. 2012. ACS Chem Biol. 7, 1152.|
|Structure formula Image|
|Primary Target||G9a and PRC2 HMTases|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
HMTase Inhibitor VI, BRD4770 - Calbiochem SDS
|Yuan, Y., et al. 2012. ACS Chem Biol. 7, 1152.|
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.