Table 2.

New putative BH3 mimetics

NameOriginTargetsBinding affinityBAX/BAK-dependent apoptosisAntitumor effects in preclinical models
BI-97D6ApoG2 atropisomerBCL-2, BCL-XL, MCL-1, A1Modest (sub μmol/L)PredominantYes
S1 derivativeSubstituted S1BCL-2, BCL-XL, MCL-1Moderate (10 nmol/L)NDNo
BH3-M6Terphenyl derivativeBCL-2, BCL-XL, MCL-1NDBAX-independentNo
BAK-dependent
PolyquinolinesQuinoline derivativesBCL-2, BCL-XL, MCL-1, A1Low (μmol/L)YesNo
MaritoclaxIsolated from marine streptomycetesMCL-1NDNDNo

Abbreviation: ND, not determined.