Bcl-2 Selective Inhibitors | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8048 ABT-199 (GDC-0199)

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

Selective Bcl-2, Ki: <0.01 nM
S1057 Obatoclax Mesylate (GX15-070)

Obatoclax (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

Selective Bcl-2, Ki: 0.22 μM
S1071 HA14-1

HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.

Selective Bcl-2, IC50: 9 μM
S1001 ABT-263 (Navitoclax)

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM, but binds more weakly to Mcl-1 and A1. Phase 2.

Pan Bcl-2, Ki: <=1 nM
S1002 ABT-737

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.

Pan Bfl-1, EC50: >10 μM; Bcl-2, EC50: 30.3 nM
S1121 TW-37

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.

Pan Bcl-2, Ki: 0.29 μM
S2812 AT101

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID. Phase 2.

Pan Bcl-2, Ki: 0.32 μM
S8061 Sabutoclax

Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

Pan Bfl-1, IC50: 0.62 μM; Bcl-2, IC50: 0.32 μM
S2448 Gambogic Acid

Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.

Pan Bfl-1, IC50: 1.06 μM; Bcl-2, IC50: 1.21 μM