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Caspase Inhibitors | Activators (7)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2228 Belnacasan (VX-765) Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.
  • Mucosal Immunol, 2015, 9(1):124-36
  • Exp Cell Res, 2016, 10.1016/j.yexcr.2016.03.009.
S2738 PAC-1 PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.
S2927 Apoptosis Activator 2 Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.
S7326 Tasisulam Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
S7023 Z-VAD-FMK Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.
  • Cancer Res, 2015, 10.1158/0008-5472.CAN-14-2199
  • PLoS One, 2015, 10(3):e0122083
  • Acta Pharmacol Sin, 2014, 35(4):531-9
S8102 Z-VAD(OH)-FMK Z-VAD(OH)-FMK is an irreversible pan-caspase inhibitor.
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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2228 Belnacasan (VX-765) <1 mg/mL 100 mg/mL 100 mg/mL
S2738 PAC-1 <1 mg/mL 78 mg/mL 16 mg/mL
S2927 Apoptosis Activator 2 <1 mg/mL 61 mg/mL <1 mg/mL
S7326 Tasisulam <1 mg/mL 83 mg/mL 83 mg/mL
S7023 Z-VAD-FMK <1 mg/mL 93 mg/mL <1 mg/mL
S8102 Z-VAD(OH)-FMK <1 mg/mL 90 mg/mL 90 mg/mL
S2448 Gambogic Acid <1 mg/mL 100 mg/mL 100 mg/mL
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