382194

HMTase Inhibitor VI, BRD4770

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

• Synonym(s): HMTase Inhibitor VI, BRD4770, 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
• MDL number: MFCD23143627
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
G9a and PRC2 HMTases

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable