| Identification | Back Directory | [Name]
2H-Benzimidazole-2-thione, 1-[2-(1H-benzimidazol-2-ylthio)ethyl]-1,3-dihydro-3-methyl- | [CAS]
433249-32-2 | [Synonyms]
2H-Benzimidazole-2-thione, 1-[2-(1H-benzimidazol-2-ylthio)ethyl]-1,3-dihydro-3-methyl- | [Molecular Formula]
C17H16N4S2 | [MOL File]
433249-32-2.mol | [Molecular Weight]
340.47 |
| Chemical Properties | Back Directory | [Boiling point ]
555.2±60.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: 50mg/mL | [form ]
solid | [pka]
10.72±0.10(Predicted) | [color ]
off-white | [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) | [InChIKey]
KDPSGIFCBZTBEZ-UHFFFAOYSA-N | [SMILES]
S=C(N(C)C1=C2C=CC=C1)N2CCSC3=NC4=C(N3)C=CC=C4 |
| Hazard Information | Back Directory | [Uses]
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- 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). |
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| Company Name: |
Merck KGaA
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| Telephone: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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