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)
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-XLin 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-xLin 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
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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