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Caspase Inhibitors | Activators (10)


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
S7312 Z-DEVD-FMK Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.
S7314 Z-IETD-FMK Z-IETD-FMK is a specific Caspase-8 inhibitor.
  • Cancer Biol Ther, 2014, 15(6):758-67
S7311 Q-VD-OPh Q-VD-OPh is a potent pan-caspase inhibitor with IC50 ranging from 25 to 400 nM for caspases 1, 3, 8, and 9, showing inhibitory effects on terminal caspase activation, substrate cleavage, and DNA ladder formation associated with apoptosis.
S8102 Z-VAD-FMK (Caspase Inhibitor VI) Z-VAD-FMK (Caspase Inhibitor VI) 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
S7312 Z-DEVD-FMK <1 mg/mL 100 mg/mL <1 mg/mL
S7314 Z-IETD-FMK <1 mg/mL 91 mg/mL <1 mg/mL
S7311 Q-VD-OPh <1 mg/mL 100 mg/mL 100 mg/mL
S8102 Z-VAD-FMK (Caspase Inhibitor VI) <1 mg/mL 90 mg/mL 90 mg/mL
S2448 Gambogic Acid <1 mg/mL 100 mg/mL 100 mg/mL
Tags: Caspases apoptosis | Caspase inhibition | Caspase activation | Caspase activity | Caspase pathway | Caspase phosphorylation | Caspase cleavage | Caspase activity assay | Procaspase activation | Caspase inhibitor in vivo | Caspase inhibitor clinical trial | Caspase-independent apoptosis | Caspase-dependent apoptosis | Caspase inhibitor review
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