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382194 Sigma-Aldrich

HMTase Inhibitor VI, BRD4770 - Calbiochem

The HMTase Inhibitor VI, BRD4770 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym: EHMT2/G9a Inhibitor VI, Methyl-2-benzamido-1-(3-phenylpropyl)-1H-benzo[d]imidazole-5-carboxylate, EHMT2/G9a Inhibitor VI, Methyl-2-benzamido-1-(3-phenylpropyl)-1H-benzo[d]imidazole-5-carboxylate

  • Empirical Formula (Hill Notation) C25H23N3O3

  • Molecular Weight 413.47

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Properties

Related Categories Bioactive Small Molecules for Epigenetic Research, Biochemicals and Reagents, Epigenetics, Histone Methylation Modulators, Molecular Biology More...
brand family   Calbiochem
feature productdata solubility   DMSO (5 mg/ml)
form   White powder
packaging   10 mg in Glass bottle (382194-10MG)
purity   ≥98% by HPLC
shipped in   ambient
storage conditions   +2C to +8C
  Ok to freeze
  Protect from light

Description

Biochem/physiol Actions

Cell permeable: yes

Primary Target
G9a and PRC2 HMTases

Reversible: 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).

Other Notes

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

Packaging

Packaged under inert gas

Warning

Standard Handling (A)

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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