197330

Bcl-2 Inhibitor - CAS 383860-03-5 - Calbiochem

The Bcl-2 Inhibitor, also referenced under CAS 383860-03-5, controls the biological activity of Bcl-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Synonym(s): Bcl-2 Inhibitor - CAS 383860-03-5 - Calbiochem, 2,9-Dimethoxy-11,12-dihydrodibenzo[c,g][1,2]-diazocine 5,6-dioxide (A) and 5,5ʹ-Dimethoxy-2,2ʹ-dinitrosobenzyl (B)
• Empirical Formula (Hill Notation): C₁₆H₁₆N₂O₄
• CAS Number: 383860-03-5
• Molecular Weight: 300.31
• UNSPSC Code: 12352200

Properties

• Assay: ≥97% (TLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: green
• solubility: DMSO: 2.5 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

Contains a mixture of two tautomers (A and B). Potent, cell-permeable Bcl-2 inhibitor that competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-X_Lin vitro (IC₅₀ = 10 µM and 7 µM, respectively). Shown to reduce cell viability (IC₅₀ = 10 µM) and growth in HL60 cells with high levels of Bcl-2 expression (IC₅₀ = 4 µM). Induces apoptosis in a dose-dependent manner in cancer cells expressing high levels of Bcl-2, but has little or no effect on cells that express low levels of Bcl-2.

Contains mixture of two tautomers (A and B). A potent, cell-permeable, Bcl-2 inhibitor that competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-x_Lin vitro (IC₅₀ = 10 µM and 7 µM, respectively). Reduces cell viability and growth in the HL-60 cell line with high Bcl-2 expression (IC₅₀ = 4 µM). Also induces apoptosis in a dose-dependent manner in cancer cells exhibiting high Bcl-2 expression with little effect on cancer cells with low Bcl-2 expression.

Biochem/physiol Actions

Cell permeable: yes

Reversible: no

Target IC₅₀: 10 µM and 7 µM for competing with Bak BH3 peptide for binding to Bcl-2 and Bcl-xL in vitro, respectively; 4 µM for reducing cell viability and growth in the HL-60 cell line with high Bcl-2 expression

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution aliquot and freeze under inert gas (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Enyedy, I.J., et al. 2001. J. Med. Chem.44, 4313.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable