For research use only. Not Intended for Therapeutic Use!
|IC50:||0.5- 2 uM |
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(+)-Apogossypol(Apogossypol; NSC736630) is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.
IC50 value: 0.5- 2 uM 
Target: Bcl-2 inhibitor
in vitro: Bcl-2-expressing B cells from transgenic mice were more sensitive to cytotoxicity induced by apogossypol than gossypol, with LD50 values of 3 to 5 microM and 7.5 to 10 microM, respectively .
in vivo: Using the maximum tolerated dose of gossypol for sequential daily dosing, apogossypol displayed superior activity to gossypol in terms of reducing splenomegaly and reducing B-cell counts in spleens of Bcl-2-transgenic mice . Apogossypol is capable of binding and inhibiting Bcl-2 and Bcl-X(L) with high affinity and induces apoptosis of tumor cell lines .
. Kitada S, et al. Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048). Blood. 2008 Mar 15;111(6):3211-9.
. Becattini B, et al. Rational design and real time, in-cell detection of the proapoptotic activity of a novel compound targeting Bcl-X(L). Chem Biol. 2004 Mar;11(3):389-95.