Catalog Number: 1541
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
  • M.Wt:
    409.23
  • Formula:
    C17H17BrN2O5
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Storage:
    Desiccate at -20°C
  • CAS No:
    65673-63-4
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.
Background References
  1. 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
  2. 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
  3. 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
Citations:

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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  1. Coeloglossum viride var. bracteatum extract protects against amyloid toxicity in rat prefrontal cortex neurons.
    Authors: Qin Et al.
    Blood 2010;3:88
  2. 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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