All Photos(2)

203830

Sigma-Aldrich

BRD2 Inhibitor II, BIC1 - Calbiochem

The BRD2 Inhibitor II, BIC1 controls the biological activity of BRD2.

Synonym(s):
1-(2-(1H-Benzimidazol-2-ylsulfanyl)ethyl)-3-methyl-1,3-dihydro-2H-benzimidazole-2-thione, 1-(2-(1H-Benzo[d]imidazol-2-ylthio)ethyl)-3-methyl-1H-benzo[d]imidazole-2(3H)-thione, BRD2 Bromodomain-Interactive Compound, BIC1, BRD2 Inhibitor II, BIC1 - Calbiochem
Empirical Formula (Hill Notation):
C17H16N4S2
Molecular Weight:
340.47
MDL number:

Quality Level

assay

≥95% (HPLC)

form

solid

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

S=C(N(C)C1=C2C=CC=C1)N2CCSC3=NC4=C(N3)C=CC=C4

General description

A cell-permeable benzimidazolyl-benzimidazolothione that targets the BD1 domain of the BET family member BRD2 (Kd = 28 µM), making it inaccessible for acetylated H4K12 (histone H4 Lys12) binding. Shown to effectively inhibit TSA- (Cat. No. 647925; 1 h 1 µM) induced BRD2 BD1-H4K12 association in COS7 cells (100% inhibition by 60 µM BIC1) and greatly suppress active Ras-induced SV40 promoter transcription activity in HeLa cells (70% inhibition by 5 µM BIC1), while being much less effective against BRDT BD1 binding to acetylated H4K5/K8.
A cell-permeable benzimidazolyl-benzimidazolothione that targets BD1 (bromodomain 1) of the BET (bromodomain and extra terminal domain) family member BRD2 (Kd = 28 µM in equilibrium binding studies by SPR, using human BRD2 aa 74-194), making it inaccessible for acetylated H4K12 (histone H4 Lys12) binding. Shown to effectively inhibit TSA- (Cat. No. 647925; 1 h 1 µM) induced BRD2 BD1-H4K12 association in COS7 cells (59% and 100% inhibition, respectively, by 10 and 60 µM BIC1) and greatly suppress active Ras-induced SV40 promoter transcriptional activation in RasV12-transfected HeLa cells (70% inhibition by 5 µM BIC1), while being much less effective against BRDT BD1 and acetylated H4K5/K8 interaction in TSA-stimulated COS7 cells (Maximum inhibition = 47% by 60 µM BIC1).

Packaging

10 mg in Glass bottle
Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Ito, T., et al. 2011. Chem. Biol.18, 495.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK Germany

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

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