BH3I-1

BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.

Product Specifications

CAS Number

[300817-68-9]

Product Name Alternative

BHI1

UNSPSC

12352005

Hazard Statement

H302+H312+H332

Target

Bcl-2 Family; E1/E2/E3 Enzyme; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BH3I-1.html

Purity

98.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(O)C(C(C)C)N(C/1=O)C(SC1=C\C2=CC=C(Br)C=C2)=S

Molecular Formula

C15H14BrNO3S2

Molecular Weight

400.31

Precautions

H302+H312+H332

References & Citations

[1]Wang L, et al. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18 (1) :236-40.|[2]Porter JR, et al. Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2. Chem Commun (Camb) . 2010 Nov 14;46 (42) :8020-2.|[3]Degterev A, et al. Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL. Nat Cell Biol. 2001 Feb;3 (2) :173-82.