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.

WF-210 is a PAC-1 derivative and potent activator of procaspases-3 with EC50 of 0.95 uM, displays more cytotoxic than PAC‐1 to human cancer cells, but less cytotoxic to normal cells; exhibits an enhanced zinc chelating ability (EC50=2.88 uM) compared to PAC‐1, activates procaspase-3 through relief of zinc-mediated inhibition; more potently induces cancer cell death in vitro with mean IC50 of 0.88 uM against 15 cancer cell lines, induces apoptosis in HL-60 and U-937 cells via a caspase-dependent pathway, activates procaspase-3, reduces IAPs, and inhibits tumor growth in breast, liver, and gallbladder xenograft tumor models.

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.

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.

Procaspase-3 activator 1541B is a specific, small molecule activator of procaspases-3 with EC50 of 1.3 uM; shows no activition activity for procaspases-6; shows considerable synergy in activating procaspase-3 in vitro combined with PAC-1, stimulates rapid and dramatic maturation of procaspase-3 in multiple cancer cell lines; effectively reduces tumor burden in a murine lymphoma model combined with PAC-1, but not treated alone.

Procaspase-3 activator 1541 is a small-molecule inducer of cell death that noncovalently self-assembles into chemical fibrils and activates procaspase-3 and 6 in vitro (EC50=2.4 and 2.8 uM); does not activate procaspases-1 or -7, induces cell death by the fibrillar rather than the soluble form of the compound; induces extensive proteolysis including caspase substrates, yet modulatory profiling reveals that chemi-fibrils form a distinct class from existing inducers of cell death.

A potent Caspase-6 inhibitor with IC50 of 192 nM, also inhibits Caspase-4/8/9/10 with IC50 of 0.1-0.8 uM; shows weak activity against other Capase subutypes; inhibits Caspase-6 in Caspase-6-transfected HCT116 cells with IC50 of 4.82 uM; inhibits serum deprivation-induced Caspase-6 activity and prevents amyloid precursor protein-mediated neurite degeneration in human primary CNS neurons; BBB penetrant.

MLT-748 (MLT748) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 5 nM, does not show inhibitory activity against 22 other tested human proteases (IC50>100 uM); binds MALT1 in the allosteric Trp580 pocket, reversibly binds and stabilizes human mutant MALT1-W580S with Kd of 13 nM, with affinity similar to that of the wild type MALT1 (Kd=42 nM); stabilizes MALT1-W580S in MALT1mut/mut B cells with EC50 of 69 nM, blocks cleavage of MALT1 substrates in human lymphocytes, including HOIL1, RelB, CYLD, and BCL10 (BCL10 cleavage IC50=31 nM), rescues MALT1 function in patient MALT1mut/mut lymphocytes.

MLT-747 (MLT747) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 14 nM; binds MALT1 in the allosteric Trp580 pocket, reversibly binds and stabilizes human mutant MALT1-W580S in vitro and in MALT1mut/mut B cells, inhibits MALT1 peptide cleavage.

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.