An inhibitor of anti-apoptotic Bcl-2 proteins

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BH3I-1

Name: BH3I-1
Brand: -

Item No. 18763

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

5-[(4-bromophenyl)methylene]-α-(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(Learn about Variance in Solubility)

DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 5 mg/ml

λ_max

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

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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1 mg

$49

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5 mg

$202

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10 mg

$354

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25 mg

$762

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Product Description

BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis.¹ 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 K_i values of 43.4 and 124 µM, respectively.^2,3 BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells.²

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Degterev, A., Lugovskoy, A., Cardone, M., et al. Identification of small-molecule inhibitors of interaction between the BH₃ domain and Bcl-xL. Nat. Cell Biol. 3(2), 173-182 (2001).

2. Roa, W., Chen, H., Alexander, A., et al. Enhancement of radiation sensitivity with BH3I-1 in non-small cell lung cancer. Clin.Invest.Med. 28(2), 55-63 (2005).

3. Porter, J.R., Helmers, M.R., Wang, P., et al. Profiling small molecule inhibitors against helix-receptor interactions: The Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2. Chem. Commun. (Camb.) 46(42), 8020-8022 (2010).

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