Ethyl [2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)]-4H-chromene-3-carboxylate Off-white to pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A small, cell-permeable nonpeptidic ligand that binds to the Bcl-2 surface pocket (IC50 = 9 µM in competition with Bcl-2 binding of Flu-BakBH3) and blocks its biological action. Induces apoptosis in HL-60 leukemic cells overexpressing Bcl-2 and in NIH 3T3 cells via the activation of caspases by a mechanism that is distinct from Fas-mediated apoptosis. Note: 1 set = 5 x 2 mg. Purity: ≥95% by elemental analysis. Ref.: Wang, J.-L., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 7124. |