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

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.

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

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)