M867 is a selective and reversible inhibitor of caspase-3 with an IC50 of 1.4 nM and Ki of 0.7 nM. M867 has anti apoptotic activity[1].
PHA-690509 is an anti-ZikV compound that inhibits ZikV replication. PHA-690509 is also a CDK inhibitor, and inhibits caspase-3 activity[1][2].
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
Euphornin is a anticaner agent, that can be isolated from E. helioscopia. Euphornin induces apoptosis via caspase-mediated pathways. Euphornin induces cell cycle arrest by increasing the level of the phospho-CDK1 (Tyr15) protein[1].
MMPSI is a potent and selective small molecule caspase 3 and caspase 7 inhibitor with an IC50 of 1.7 μM for human caspase-3. MMPSI can significantly reduce ischemia-reperfusion-induced infarct size in the isolated rabbit heart, and reduce apoptosis in both the ischemic myocardium and isolated cardiomyocytes. MMPSI can be used for researching cardioprotection[1].
Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex[1]. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt[2]. Anti-cancer, anti-inflammatory, and antioxidant activities[3].
CZL55 is a caspase-1 inhibitor with an IC50 value of 24 nM. CZL55 can be used for the research of febrile seizures (FS)[1].
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].non-alcoholic fatty liver disease[1][2][3].
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells[1].
Z-VDVAD-FMK is a special inhibitor of caspase-2. Z-VDVAD-FMK produces a reduction in Lovastatin-induced apoptosis[1][3][3].
Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research[1].
Z-IETD-FMK is a selective and cell permeable caspase 8 inhibitor.
Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage.Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway[1].
Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium, which exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8[1][2].
Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells[1]. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo[2].
Chelidonic acid is a component of Chelidonium majus L., used as a mild analgesic, an antimicrobial, an acentral nervous system sedative. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1[1]. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM[2].
AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.
Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer[1][2].
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2].
Z-VEID-FMK is a selective inhibitor of caspase-6. Z-VEID-FMK can be used for the research of tumor[1].
Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with IC50 of 18 μM.
Frondoside A, a natural glycoside extracted from the sea cucumber, Cucumaria frondosa, possesses anticancer, anti-invasive, anti-metastasis, anti-angiogenic and pro-apoptosis properties with high safety[1][2].
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development[1][2][3].
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) [1][2][3].
Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity[1].
M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability[1].
Ac-YVAD-AOM is the inhibitor of caspase-1 that shows antitumor activity[1].
Caspase-8-IN-1 is a potent caspase-8 inhibitor[1].
Z-LEED-FMK is a caspase-13 and caspase-4 inhibitor. Z-LEED-FMK also inhibits caspase-1 processing in S. typhimurium-infected macrophages[1][2].
Taurochenodeoxycholic acid is one of the main bioactive substances of animals' bile acid.