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HA-14-1 is a small molecule that binds the surface pocket of Bcl-2 proteins (IC₅₀ = ~ 9 μM) and induces apoptosis by interfering with its interaction with the Bak peptide and activating Apaf-1 and caspase-9 and -3.¹ It can also bind to the antiapoptotic Bcl-2 proteins Bcl-xl and Bcl-W.² HA-14-1 has been shown to induce apoptosis of human acute myeloid leukemia (HL-60) cells (50 μM induces 90% loss of viability).¹

(Rac)-HA14-1 is the racemic form of HA14-1 (HY-12011). HA14-1 is a Bcl-2/Bcl-xL antagonist with an IC50 of approximately 9 μM against Bcl-2[1].

ChEBI: 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-1-benzopyran-3-carboxylic acid ethyl ester is a 1-benzopyran.

1. Wang, J.L., Liu, D., Zhang, Z.J., et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells Proc. Natl. Acad. Sci. USA 97(13),7124-7129(2000).
2. Azmi, A.S., and Mohammad, R.M. Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy J. Cell Physiol. 218(1),13-21(2009).