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KEA1-97 (KEA 1-97) is a small molecule that disrupts the interaction of thioredoxin with caspase 3; activates caspases, and induces apoptosis without affecting thioredoxin activity, impairs triple-negative breast cancer cell survival; impairs in vivo breast tumor xenograft growth.


MALT1 paracaspase inhibitor 3

2088355-90-0 MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk; binds covalently to the catalytic cysteine (C464) of MALT1, induces MALT1 oligomerization; exhibits potent activity in the Raji-GloSensor MALT1 protease inhibition (IC50=60 nM) and OCI-Ly3 growth inhibition assays (IC50=0.1 uM), selectively inhibits the growth of MALT1 dependent cell lines by decreasing cell proliferation and increasing apoptosis; downregulated IL10 protein expression in vitro and in vivo, also decreases STAT3 phosphorylation in ABC DLBCL cells; suppresses the growth of ABC DLBCL tumors in vivo.


1230628-71-3 ML132 (NCGC-00183434, CID-4462093) is a highly potent, selective Caspase 1 inhibitor with IC50 of 0.023 nM, displays >1,000-fold selectivity over a panel of 9 caspases.


634911-80-1 BOC-D-FMK is a cell-permeable, irreversible, broad spectrum caspase inhibitor, inhibits apoptosis stimulated by TNF-α with IC50 of 39 uM; inhibits TNFα-stimulated reactive oxygen species (ROS) generation, prevents genistein-induced apoptosis of p815 cells at 50 uM; shows neuroprotective effects on spinal motoneurons (MNs) after root avulsion in neonatal rats, suppresses polyethylene particle-induced osteolysis in mice.


273404-37-8 VX-765 (Belnacasan) is an orally absorbed prodrug of VRT-043198, which is a potent and selective inhibitor of interleukin-converting enzyme/caspase-1 with Ki of 0.8 nM; VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9, VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases; inhibits LPS-induced IL-1β production, reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation.


Phase 2 Discontinued



210344-95-9 Z-DEVD-FMK is a specific caspase-3 inhibitor with IC50 of 18 uM; affects the survival and function of platelets in platelet concentrate during storage, blocks the geranylgeraniol-induced DNA fragmentation in human leukemia cells; abolishes the apoptosis, CPP32/Mch3alpha processing and the increase in CPP32-like protease activity induced by TGF-beta1 in rat hepatocytes.


1135695-98-5 Q-VD-Oph is a potent pan-caspase inhibitor, inhibits human recombinant caspase-7 with IC50 of 48 nM in cell-free assay, also inhibits caspase -1, 3, 8, 9, 10, and 12 with IC50 of 25-400 nM; reduces doxorubicin-induced caspase-3 activation, increases expression of p21/WAF1 and senescence -associated -beta-galactosidase activity, but does not alter Akt activation, Q-VD-Oph is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk; prevents activated caspase-7 and caspase-cleaved fragments of tau in the TgCRND8 brain, as well as pathology associated with TgCRND8 mice.

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