Table 1.

Previously characterized BH3 mimetics

NameOriginBH3 mimicryBH3 mimeticIn vivo antitumor effects in animal modelsClinical trials
ABT-737Small organic moleculeBAD-likeAuthenticYesNo
ABT-263/navitoclaxABT-737 derivativeBAD-likeAuthenticYesYes
ObatoclaxDerivative of natural progidiosinPan-BH3-onlyPutative/off-target effectsYesYes
GossypolPlant-derived polyphenolPan-BH3-onlyPartial/off-target effectsYesYes
AT-101Gossypol isomerPan-BH3-onlyPartial/off-target effectsYesYes
ApogossypolGossypol derivativePan-BH3-onlyPartial/off-target effectsNDNo
Apogossypolone/ApoG2AT-101 derivativePan-BH3-onlyPartial/off-target effectsYesNo
BI-97C1/sabutoclaxApogossypol derivativePan-BH3-onlyPartial/off-target effectsYesNo
TW37Gossypol analogPan-BH3-onlyPartial/off-target effectsYesYes
S1Heterocyclic compoundPan-BH3-onlyPartial/off-target effectsYesNo
072RBBIM BH3-derived peptidePan-BH3-onlyPutativeYesNo
SAHB-ABID BH3-derived SAHBBAD-likePutativeYesNo
BIMS2ABIM BH3 mutantNOXA-likeAuthenticYesNo
Mcl-1 SAHBMCL-1 BH3-derived SAHBNOXA-likeAuthenticNDNo

Abbreviations: BH3, BCL-2 homology domain 3; ND, not determined.