Cell-permeable inhibitor of Bcl-2 protein (IC50
~ 9 μ
M); acts by binding to the surface pocket. Disrupts Bax/Bcl-2 interaction and induces apoptosis of tumor cells. Also binds to the antiapoptotic Blc-2 proteins Bcl-XL and Bcl-w.
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Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
Doshi et al.
Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia.
Milella et al.
Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells.
Wang et al.
The citations listed below are publications that use Tocris products. Selected citations for HA14-1 include:
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