Cat. No. 1541

HA14-1 C17H17BrN2O5 [65673-63-4]

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Chemical Name: 2-Amino-6-bromo-α-cyano-3-(ethoxycarbonyl)-4H-1-benzopyran-4-acetic acid ethyl ester

Biological Activity

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

Soluble to 100 mM in DMSO and to 100 mM in ethanol
Desiccate at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Doshi et al (2006) 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. J.Med.Chem. 49 7731. PMID: 17181155.

Milella et al (2002) Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia. Blood 99 3461. PMID: 11964319.

Wang et al (2000) Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc.Natl.Acad.Sci.U.S.A. 97 7124. PMID: 10860979.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for HA14-1 include:

Qin et al (2010) Coeloglossum viride var. bracteatum extract protects against amyloid toxicity in rat prefrontal cortex neurons. Blood 3 88. PMID: 20369044.

Mohan et al (2009) 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. Brain Res 1283 155. PMID: 19505441.

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Keywords: HA14-1, supplier, Bcl-2, inhibitors, inhibits, induces, apoptosis, Bax, Bcl-XL, Mcl-1, Family, bcl2, inhibitor, Tocris Bioscience, Bcl-2 Family Inhibitor products

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