Caspase

Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

Z-VAD(OMe)-FMK is a pan-caspase inhibitor with irreversible properties; Z-VAD(OMe)-FMK is also an inhibitor of ubiquitin C terminal hydrolase L1 (UCHL1), which is irreversibly modified by targeting the UCHL1 active site.

Emricasan (IDN-6556) is a pan-caspase inhibitor with irreversible properties. Emricasan has anti-inflammatory and anti-apoptotic activity and can be used in the treatment of infections and liver failure, etc. Emricasan also inhibits Zika virus infections.

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.

Z-DEVD-FMK (Caspase-3 Inhibitor) is a selective, irreversible Caspase-3 inhibitor, and also exhibits effective inhibition activity on caspase-6, caspase-7, caspase-8, and caspase-10.

Q-VD-OPH (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a pan-caspase inhibitor with potent antiapoptotic properties.

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a cell-permeable, selective inhibitor of caspase 8.

MJN68390 has an apparent IC50 value of 15 μM against CASP8 and shows no activity against CASP10.

Ac-FLTD-CMK is an inhibitor derived from abscisicin D (GSDMDD) with specific inhibitory effects on inflammatory caspases. ac-FLTD-CMK showed inhibitory effects on caspases-1, caspases-4 and caspases-11 with IC50s of 46.7 nM, 1.49 μM and 329 nM, respectively. Ac-FLTD-CMK showed potency against caspases-1, caspases-4 and caspases-11, but not against apoptosis-associated caspase-3.

Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

AA-Z-YVAD-FMK is a Irreversible caspase-1 inhibitor,with anti-inflammatory and anti-tumor activities.

Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) is a selective and irreversible inhibitor of Caspase-1 and inhibits pyroptosis, IL-1β and IL-18. Ac-YVAD-CMK shows neuroprotective and anti-inflammatory capacity.

Se-Methylselenocysteine (Se-MSC) is a potent chemopreventive agent in many test systems and has been shown to inhibit tumor promotion and induce apoptosis.

Belnacasan (VX-765) is an orally active inhibitor of IL-converting enzyme caspase-1.

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

Ac-DEVD-CHO is a specific Caspase-3 inhibitor (Ki: 230 pM) with inhibitory effects on SLNT-induced apoptosis.

Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 Ki: 3.4 0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31 3500 nM).

Z-LEHD-FMK is a selective and potent caspase-9 inhibitor that protects against reperfusion injury and slows apoptosis. Z-LEHD-FMK exhibits antitumor and neuroprotective activity, increases the yield of in vitro-produced preimplantation embryos of [Bubalus bubalis], and alters the cellular stress response.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

1. Soyasaponin Bb (Soyasaponin I) can suppress Eca-976 cell growth, reverse effects on over expression of c-met, VEGF, and induce cell apoptosis through inhibiting HDAC1-NF-kappaB and activating PETEN and caspase-3 signaling pathways.

Lasiodin (Lasiokaurin) is a diterpene compound from the plant Camellia sinensis that inhibits the proliferation of NPC cells. Lasiodin has antioxidant, antitumor and antibacterial activities, induces cell cycle length and apoptosis, induces cell migration and invasion, and can be used in the study of nasopharyngeal carcinoma.

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

Licochalcone A is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch with obvious anti-cancer effects.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

Ginsenoside Rh2 (20(S)-Ginsenoside Rh2), an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.

SDZ 224-015 is an orally active inhibitor of interleukin-1β (IL-1β) converting enzyme and caspase-1, exhibiting anti-COVID-19 and anti-inflammatory activity, and reducing carrageenan gum-induced paw edema in rats.

Boc-D-FMK is an irreversible, cell-permeable, and broad-spectrum caspase inhibitor and inhibits apoptosis stimulated by TNF-α (IC50: 39 µM).

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

1.Aristolactam I (Aristololactum) has cytotoxic potency, mediated through the induction of apoptosis in a caspase 3-dependent pathway. 2. The effects of Aristololactam I may be mediated by different mechanisms except TGF-beta1 pathway. 3. Aristololactam I may be one of toxic metabolites in Chinese herbs containing AA which participate in renal damage and fibrosis.

Formosanin C (Polyphyllin B) is a compound isolated from Rhizoma Paridis, showed pro-apoptosis and immunoregulation with antitumor activity in cultured cells and animal systems.

PAC-1 (Procaspase activating compound 1) has been used in trials studying the treatment of Lymphoma, Melanoma, Solid Tumors, Breast Cancer, and Thoracic Cancers, among others.

Effusol is a natural product, exhibits potent scavenging activity for DPPH and ABTS radicals(IC50 values of 79 μM and 2.73 μM, respectively). Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline. Effusol can induce caspase-3-mediated cytotoxicity in HT22 cells.

Raptinal activates caspase-3 directly and initiates intrinsic caspase-dependent apoptosis pathway in multiple cell lines.

Crustecdysone (Hydroxyecdysone) is a steroid hormone that regulates the processes of molting or ecdysis in insects.

Zingiberen newsaponin is a steroidal saponin from Dioscorea zingiberensis.

Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities.

Penicillic acid, a polyketide mycotoxin, synthesized by various species of Aspergillus and Penicillium, acts as an inhibitor of Fas ligand-induced apoptosis by impeding self-processing of caspase-8. Additionally, in vitro studies have shown that Penicillic acid displays cytotoxic properties in rat alveolar macrophages.

Dihydrosanguinarine, a natural compound isolated from the leaves of [Macleaya microcarpa], exhibits antifungal and anticancer activity.

1. Senkyunolide I has neuroprotective effect, associated with its anti-oxidation and anti-apoptosis properties.

Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.

Caspase-3 Inhibitor I (N-acetyl-asp-glu-val-asp-al) is a specific inhibitor of Caspase-3.

Fenbufen (Lederfen) is a non-steroidal anti-inflammatory drug used primarily to treat inflammation in osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve backaches, sprains, and fractures. Fenbufen is available as a capsule or tablet sold with the brand names Cepal, Cinopal, Cybufen, Lederfen, and Reugast. Fenbufen acts by preventing cyclooxygenase from producing prostaglandins which can cause inflammation.

Apoptosis Inhibitor was a novel inhibitor of programmed cell death associate with caspase-3 inhibition.

Polyporenic acid C shows inhibitory activity against human collagenase.

1. Sesamolin and Sesamin has neuroprotective effect. 2. Sesamolin protects microglia against H2O2-induced cell injury, by inhibiting of p38 MAPK and caspase-3 activation and ROS production. 3. Sesamolin and Sesamin can significantly attenuate the excess g

Puerarin 6''-O-xyloside possesses significant anti-osteoporotic activity on ovariectomy mice, it has significant antitumour activities, the mechanisms are related to increased levels of caspase-3, caspase-7, caspase-9 and Bax, and reduced levels Bcl-2.

Gardenin B exhibits superior antiproliferative activity against lung, breast, colon, hepatic and leukaemia cell lines as well as in keratinocytes .