Table 1Summary of inhibitor potencies for all six antiapoptotic human Bcl-2-family proteins by fluorescence polarization (FPA) with GST-Bcl-2 fusion proteins and FITC-Bid BH3 peptide

Potency [IC50 (μM)] against Individual Bcl-2 proteins
CompoundBcl-BBcl-XLBcl-2Bcl-WBfl-1Mcl-1Ref
(−)-Epigallocatechin gallate (EGCG)0.360.590.452.331.790.921
Gossypol0.163.030.281.4>101.751
Apogossypol0.372.800.642.10>103.351
Obatoclax* (GX15-070),2.154.691.117.015.002.901
ABT-737 (enantiomer of ABT-263)>100.0640.120.024>20>201
Sabutoclax (BI-97C1 - an optically pure apogossypol derivative of BI-79D10),-0.310.32-0.620.203**
*

Navitoclax* (ABT-263) was not tested against Bcl-B & Bfl-1 [2]; values reported as Ki for different peptide/protein pairs so conversion to comparable IC50s difficult; however, it is pan-inhibitory within 2-fold for Bcl-XL, Bcl-2, Bcl-W & Mcl-1

**

References 11 & 12 therein; discrepant reported values, but confirm pan-inhibition for Bcl-XL, Bcl-2, Bcl-W & Mcl-1

From: Selective Bcl-2 Inhibitor Probes

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