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MIK665 (S-64315, MIK-665) is a novel potent, selective Mcl-1 inhibitor with potential pro-apoptotic and antineoplastic activities; binds to and inhibits the activity of Mcl-1, which promotes apoptosis of cells overexpressing Mcl-1. Mcl-1, an anti-apoptotic protein belonging to the Bcl-2 family of proteins, is upregulated in cancer cells and promotes tumor cell survival.

Blood Cancer

Phase 1 Clinical




S55746 (BCL201, Servier-1) is a novel potent, selective, orally bioavailable inhibitor of BCL-2 with Ki of 1.3 nM, 70- 400 fold selectivity over BCL-XL, on significant binding to MCL-1 and BFL-1; potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM, exhibits a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line; concentration-dependently disrupts the BCL-2/BAX complex in RS4;11 cells, selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner; induces cell death in a panel of non-Hodgkin lymphoma cells; inhibits xenograft growth in RS4;11 and Toledo models.

Blood Cancer

Phase 1 Clinical


Mcl-1-Puma inhibitor 8


Mcl-1-Puma inhibitor 8 is a small-molecule dual-acting compound that targets the apoptotic Mcl-1-PUMA interface with Ki of 0.3 uM (Mcl-1, FPA), reduces multiple cancer cells and inhibits PUMA-mediated apoptosis; a useful chemical probe to achieve safer cancer therapies by modulating Mcl-1-PUMA interaction.




BCL6-IN-8 (BCL6-i) is a potent, irreversible and cell-active BCL6 inhibitor with inact/KI value of 1.9 × 104 M-1 s-1, targets Cys53 located at the protein-protein interaction interface; shows intracellular PPI inhibitory activity between BCL6 and its corepressors, thus resulting in BCL6-dependent DLBCL cell growth inhibition; BCL6-i is a cell-active chemical probe with the most potent BCL6 inhibitory activity reported to date.


AZD 5991


AZD 5991 (AZD5991) is a potent and selective macrocyclic inhibitor of Mcl-1 with sub-nanomolar affinity; promotes rapid apoptosis in Mcl-1-dependent cell lines (GI50=10 nM in multiple myeloma cell lines), disrupts Mcl-1/Bak complex; completely causes tumor regression in several mouse xenograft models after a single tolerated dose.

Blood Cancer

Phase 1 Clinical


(-) BI97D6


(-) BI97D6 (BI112D1) is a potent, pan-active inhibitor of Bcl-2 family proteins with IC50 of 76, 31, 25, and 122 nM for Bcl-xL, Bcl-2, Mcl-1, and Bfl-1, respectively; effectively inhibits cell growth in the PC-3 human prostate cancer and H23 human lung cancer cell lines with EC50 of 0.22 and 0.14  uM, respectively; effectively induces apoptosis in the BP3 human lymphoma cell line; displays in vivo efficacy in a prostate cancer xenograft model in mice; also overcomes ABT-737 resistance in AML, kills AML leukemia stem/progenitor cells while largely sparing normal hematopoietic stem/progenitor cells.




BI-3802 (BI3802) is a highly potent and efficacious BCL6 degrader that potently inhibits the interaction of the BTB/POZ domain of BCL6 with several co-repressors in vitro with IC50 of <3 nM; inhibits the BCL6/Co-repressor complex formation with IC50 of 43 nM in vitro, also is a potent and efficacious degrader of the BCL6 protein in many DLBCL cell lines (DC50=20 nM in SU-DHL-4 cells); BI-3802 is a valuable probe compound for testing hypotheses around BCL6 biology.

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