Epigenetic Multiple Ligand

References
Mai, A., et al. 2008. J. Med. Chem. 51, 2279.

URL

http://eshop.emdchemicals.com/products/EMD_BIO-324888?WT.mc_id=EB000129">Epigenetic Multiple Ligand

CAS Number

Empiracal formula

C₁₉H₁₂Br₄O₄

Form Light orange solid

Formulation

Description

A cell-permeable bis-arylidene compound that acts as an epigenetic multiple ligand (epi-ML) and inhibits substrates processing by several chromatin-associated enzymes, including H4/PRMT1 (91% inhibition at 50 µM), H4/RmtA (50% inhibition at 29 µM), H3/p300/CBP (61% inhibition at 50 µM), PABP1/CARM1 (>90% inhibition at 100 µM), H3/SET7 (>90% inhibition at 100 µM), SIRT1/2 (>50% inhibition at 25 µM), although the process of Np13p by PRMT1 is only weakly affected. Shown to induce either apoptosis (28% after 30 h incubation with 25 µM inhibitor) or granulocytic differentiation (100% of non-apoptotic cells after 30 hr incubation with 5 µM inhibitor) among U937 cell population.

Molecular weight

623.9

Purity ≥97% by HPLC

R phrase

RTECS

Solubility DMSO

Primary target

Primary target IC50