BH3I-1

The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains. BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis. It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively. BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.Formal Name: 5-[(4-bromophenyl)methylene]-alpha-(1-methylethyl)-4-oxo-2-thioxo-3-thiazolidineacetic acid. CAS Number: 300817-68-9. Molecular Formula: C15H14BrNO3S2. Formula Weight: 400.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 279, 382 nm. SMILES: BrC1=CC=C(/C=C2C(N(C(C(O)=O)C(C)C)C(S\2)=S)=O)C=C1. InChi Code: InChI=1S/C15H14BrNO3S2/c1-8(2)12(14(19)20)17-13(18)11(22-15(17)21)7-9-3-5-10(16)6-4-9/h3-8,12H,1-2H3,(H,19,20)/b11-7+. InChi Key: COHIEJLWRGREHV-YRNVUSSQSA-N.