HA14-1
Chemical Name: 2-Amino-6-bromo-α-cyano-3-(ethoxycarbonyl)-4H-1-benzopyran-4-acetic acid ethyl ester
Biological Activity
HA14-1 is a cell-permeable inhibitor of Bcl-2 protein (IC50 ~ 9 μM); 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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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.
J.Med.Chem., 2006;49:7731 -
Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia.
Milella et al.
Blood, 2002;99:3461 -
Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells.
Wang et al.
Proc.Natl.Acad.Sci.U.S.A., 2000;97:7124
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Citations for HA14-1
The citations listed below are publications that use Tocris products. Selected citations for HA14-1 include:
2 Citations: Showing 1 - 2
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Coeloglossum viride var. bracteatum extract protects against amyloid toxicity in rat prefrontal cortex neurons.
Authors: Qin Et al.
Blood 2010;3:88
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Bcl-2 inhibitor HA14-1 and genistein together adeptly down regulated survival factors and activated cysteine proteases for apoptosis in human malignant neuroblastoma SK-N-BE2 and SH-SY5Y cells.
Authors: Mohan Et al.
Brain Res 2009;1283:155
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