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.

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.

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

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

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

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.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

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

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

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

Ac-YVAD-AOM is a selective and potent caspase-1 inhibitor showing antitumor activity and potential analgesic activity.

Epieriocalyxin A can suppress Caco-2 colon cancer cell growth. It could be a potential drug for colon cancer therapy in the future.

EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway.

EP1013 is a broad-spectrum selective inhibitor of Caspase used in the study of type 1 diabetes.

Tauroursodeoxycholate sodium (TUDC) is an endoplasmic reticulum (ER) stress inhibitor, used for the treatment of gallstones and liver cirrhosis.

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

Taurochenodeoxycholic Acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid.

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

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

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

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.

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.

Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa,and has antifungal and anticancer activity.

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).

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.

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, and 3beta-O-trans-p-coumaroyltormentic acid are weakly selective for vancomycin-resistant Enterococcus (VRE) compared with eukaryotic cells, with an MIC of 59.4microg/mL and a 50% inhibitory concentration (IC50) of 72.0microg/mL for monkey kidney epithelial (MA104) cells. A mixture of 3-O-cis-p-coumaroyltormentic acid and 3-O-trans-p-coumaroyltormentic acid shows an inhibitory effect comparable to (-)-epigallocatechin gallate (EGCG) of green tea on the activation of Epstein-Barr virus early antigen (EBV-EA) induced by 12-O-tetradeca--noylphorbol-13-acetate (TPA).

Quinovic acid shows some anti-tumour activities, quinovic acid glycosides have a potent inhibitory effect on the growth of human bladder cancer cell lines by inducing apoptosis through modulation of NF-κB.

Ergosta-4,6,8(14),22-tetraen-3-one has cytotoxic activity against human gastric cancer cell, it can induce G2/M cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells, these results would be useful for the further utilization of man

Kuguaglycoside C induces caspase-independent cell death, and is involved, at least in part, in the mechanism underlying cell necroptosis.

(-)-Centrolobol has antifibrotic activity, it can significantly inhibit the proliferation of HSC-T6 cells in a dose-dependent manner. Centrolobol exhibits strong cytotoxic activity against KB cell line.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

Sageone represents a promising anticancer agent against gastric cancer that warrants further study, it synergizes with cisplatin cytotoxicity in SNU-1 human gastric cancer cells.Sageone also shows antiviral activity.

Liriodenine is a potent inhibitor of topoisomerase II (EC 5.99.1.3) both in vivo and in vitro, it has antitumor, antibacterial and antifungal activities, it can suppress ventricular arrhythmias induced by myocardial ischaemia reperfusion, through inhibiti

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.

Santamarine has significant anticancer activity, can inhibit L1210 cells because of its cytotoxic,cytostatic and blocking mitosis and reducing uptake of thymidine. Santamarine and reynosin show bactericidal activity against clinical strains of Mycobacterium tuberculosis.

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic activity with IC50 values of 42.89 μM and 33.61 μM, respectively [1].

Caspase-3 Activator 2 (Compound 2f) is a caspase 3 activator with cytotoxic effects on HL-60 and K562 cells, exhibiting IC 50 values of 33.52 μM and 76.90 μM, respectively [1]. It facilitates apoptosis, rendering it useful in cancer research.

(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell

Cedrusin shows a cytotoxic effect on A375 and HeLa cells.

Myricanol can elicit growth inhibitory and cytotoxic effects on lung cancer cells, it can significantly decelerate tumor growth in vivo by inducing apoptosis.

Scutebarbatine A shows significant antitumor effects on A549 cells in vivo and in vitro via mitochondria-mediated apoptosis by up-regulating expressions of caspase-3 and 9, and down-regulating Bcl-2. Scutebarbatine A and barbatine A show a significant ability to protect cells against H2O2 with ED50 values of 5.0 and 16.8 μM, respectively.

17-Hydroxy sprengerinin C is a glycoside compound isolated from rhizomes of Polygonatum sibiricum with stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.

Crenulatin has dual- direction effects on apoptosis of cerebral microvascular endothelial cells, inhibitive effect in 25 mg/L and stimulative effect in 100 mg/L group, respectively; the mechanism is related to the alterations of Fas/Bcl-2 expression and caspase-3 activity.

Effusanin E shows antibacterial and anti-cancer activities, it significantly inhibits cell proliferation and induces apoptosis in NPC cells by suppressing p50/p65 proteins to down-regulate COX-2 expression .

Panaxynol is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation.