DC Chemicals Limited
China
Product Name: BH3I-1
Price: $350.0/100mg $600.0/250mg $1350.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

300817-68-9

300817-68-9 structure

300817-68-9 structure

Name: BH3I-1
Chemical Name: bh3i-1
CAS Number: 300817-68-9
Molecular Formula: C₁₅H₁₄BrNO₃S₂
Molecular Weight: 400.31100
Catalog: Signaling Pathways Apoptosis Bcl-2 Family
Create Date: 2017-04-07 22:17:10
Modify Date: 2024-01-07 14:24:14
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.

Name	bh3i-1
Synonyms	5-(p-bromobenzylidene)-a-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid 5-(p-bromobenzylidene)-alpha-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid

Description	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.
Related Catalog	Signaling Pathways >> Apoptosis >> Bcl-2 Family Signaling Pathways >> Apoptosis >> MDM-2/p53 Research Areas >> Cancer
Target	Bcl-2 Bcl-xL Bak Bim p53/mDM2:5.3 μM (Kd)
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[2]. 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[3].
Cell Assay	Jurkat cells overexpressing Bcl-xL, FL 5.12 and FL 5.12/Bcl-xL cells (5×104 cells per well) are seeded into white 96-well plates and treated with various concentrations of the compounds (e.g., BH3I-1; 30 μM and 90 μM)for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 μM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay with a Victor plate reader. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 μg/mL PI. Cell death is determined by FACS analysis in a FACSCalibur machine[3].
References	[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.

Molecular Formula	C₁₅H₁₄BrNO₃S₂
Molecular Weight	400.31100
Exact Mass	398.96000
PSA	115.00000
LogP	3.69740
Storage condition	-20℃

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H312-H332
Precautionary Statements	P280
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Risk Phrases	20/21/22
Safety Phrases	36
RIDADR	NONH for all modes of transport