BH3I-1

SKU: orb1225390

Description

A small-molecule Bcl-2 antagonist that inhibits the ineraction of Bak BH3 and Bcl-xL with Ki of 2.4 uM in FP binding assay; specifically blocks the BH3-domain-mediated heterodimerization between Bcl-2 family members in vitro and in vivo and induces apoptosis; also potently inhibits p53/hDM2 with Kd of 5.3 uM.

Key Properties

• CAS Number: 300817-68-9
• MW: 400.3105
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₄BrNO₃S₂
• SMILES: O=C(O)C(C(C)C)N(C/1=O)C(SC1=C\C2=CC=C(Br)C=C2)=S
• Target: Bcl-2
• Solubility: DMSO: ≥ 3.9 mg/mL

Bioactivity

• In Vitro:
  BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a Kd=5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a Ki of 7.8±0.9 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BHI1 | BHI-1 | BHI 1 | BH 3I1

Quick Database Links

Gene Symbol

Bcl-2