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203830

BRD2 Inhibitor II, BIC1

Name: BRD2 Inhibitor II, BIC1
Brand: MM

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

Synonym(s):

BRD2 Inhibitor II, BIC1, 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

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About This Item

Empirical Formula (Hill Notation):

C₁₇H₁₆N₄S₂

CAS Number:

433249-32-2

Molecular Weight:

340.47

UNSPSC Code:

12352200

NACRES:

NA.28

MDL number:

MFCD03034582

Assay:

≥95% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

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

InChI

1S/C17H16N4S2/c1-20-14-8-4-5-9-15(14)21(17(20)22)10-11-23-16-18-12-6-2-3-7-13(12)19-16/h2-9H,10-11H2,1H3,(H,18,19)

InChI key

KDPSGIFCBZTBEZ-UHFFFAOYSA-N

Description

General description

A cell-permeable benzimidazolyl-benzimidazolothione that targets BD1 (bromodomain 1) of the BET (bromodomain and extra terminal domain) family member BRD2 (K_d = 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

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Regulatory Review (Z)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c