203830

BRD2 Inhibitor II, BIC1

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

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₇H₁₆N₄S₂
• CAS-Nummer: 433249-32-2
• Molekulargewicht: 340.47
• MDL-Nummer: MFCD03034582
• UNSPSC-Code: 12352200
• NACRES: NA.28

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 50 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C
• SMILES String: S=C(N(C)C1=C2C=CC=C1)N2CCSC3=NC4=C(N3)C=CC=C4

Beschreibung

Allgemeine Beschreibung

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).

A cell-permeable benzimidazolyl-benzimidazolothione that targets the BD1 domain of the BET family member BRD2 (K_d = 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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Regulatory Review (Z)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable