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
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About This Item
Empirical Formula (Hill Notation):
C25H23N3O3
Molecular Weight:
413.47
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
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
G9a and PRC2 HMTases
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
Yuan, Y., et al. 2012. ACS Chem Biol.7, 1152.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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