324888

Epigenetic Multiple Ligand

A cell-permeable bis-arylidene compound that acts as an epigenetic multiple ligand (epi-ML) and inhibits substrates processing by several chromatin-associated enzymes.

• Synonym(s): Epigenetic Multiple Ligand, 3,5-bis(3,5-Dibromo-4-hydroxybenzylidene)-tetrahydro-2H-pyran-4-one, PRMT Inhibitor IV
• Empirical Formula (Hill Notation): C₁₉H₁₂Br₄O₄
• CAS Number: 1020399-52-3
• Molecular Weight: 623.91
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light orange
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General 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 h incubation with 5 µM inhibitor) among U937 cell population.

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable