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HMTase Inhibitor III, BIX-01338

Name: HMTase Inhibitor III, BIX-01338
Brand: MM

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

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About This Item

Empirical Formula (Hill Notation):

C₃₂H₂₄F₃N₃O₆ · xH₂O

Molecular Weight:

603.54 (anhydrous basis)

UNSPSC Code:

12352200

Assay:

≥97% (HPLC)

Form:

powder

Storage condition:

OK to freeze, desiccated (hygroscopic), protect from light

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Properties

Quality Segment

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c