539212

HMTase Inhibitor III, BIX-01338

The Protein Methyltransferase Inhibitor II, BIX-01338 controls the biological activity of Protein Methyltransferase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): HMTase Inhibitor III, BIX-01338, EHMT1/GLP Inhibitor I, EHMT2/G9a Inhibitor III, 1-(4-(4-methoxybenzoyloxy)phenethyl)-2-(4-(trifluoromethyl)benzamido)-1H-benzo[d]imidazole-5-carboxylic acid, Hydrate, 1-(2-(4-(4-Methoxybenzoyloxy)phenyl)ethyl)-2-(4-trifluoromethylbenzoylamino)-1H-benzoim
• Empirical Formula (Hill Notation): C₃₂H₂₄F₃N₃O₆ · xH₂O
• Molecular Weight: 603.54 (anhydrous basis)
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O=C(C1=CC=C(C=C1)C(F)(F)F)NC2=NC3=C(N2CCC4=CC=C(OC(C5=CC=C(C=C5)OC)=O)C=C4)C=CC(C(O)=O)=C3.[xH2O]

Description

General description

A cell-permable amino-benzimidazolo compound that inhibits a broad-spectrum of histone methyltransferases, including PRMT1, SET7/9, G9a, SUV39H1, and GLP (effective conc. = 15 µM) in a SAM-competitive manner. BIX-01338 is reported to affect the growth of mES, MEF, and HeLa cells at concentrations needed for HMT inhibition, limiting its use in HMTase studies to cell-free systems only.

A cell-permeable amino-benzimidazolo compound that is shown to inhibit a broad-spectrum of histone methyltransferases, including the PRMT1 H4R3 me2 activity, SET7/9 H3K4 me activity, G9a H3K9 me2 activity, as well as the H3K9 me3 activity of SUV39H1 (wild-type and H320R hyperactive mutant) and GLP (effective conc. = 15 µM) in a SAM-competitive manner. BIX-01338 is reported to affect the growth of mES, MEF, and HeLa cells at 13.3 µM, while failing to affect cellular H3K9me/me2/me3 and H3K27me2 levels at a lower non-cytotoxic concentration of 3.3 µM, limiting its use in HMTase studies to cell-free systems only.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Other Notes

Kubicek, S., et al. 2007. Mol. Cell25, 473.

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