caspase

Q-VD-OPh is an irreversible caspase inhibitor with an IC₅₀ value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier.

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.

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.

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.

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.

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

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.

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC₅₀ = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

Boc-Asp(OMe)-fluoromethyl ketone (Boc-Asp(OMe)-FMK) is a broad range caspase inhibitor. Boc-Asp(OME)-Fluoromethyl Ketone inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

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.

Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC₅₀: 7.67 μM), PKA (IC₅₀: 9.33 μM), and PKC (IC₅₀: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

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

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

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.

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

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.

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

SACLAC is a cysteine asparaginase activation inhibitor with antitumor activity that decreases AML cell viability, inhibits AML cell proliferation, increases AML cell death, and induces apoptosis of AML cells, and is used in the study of acute myeloid leukemia and cancer.

Biotin-VAD-FMK is a cell-permeable, irreversible biotin-labeled inhibitor of caspase. It is used to identify active caspases in cell lysates.

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

Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid exhibiting anti-inflammatory and anti-cancer activities and can enhance the activation of p38 MAPK.

Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC₅₀ = 23 nM) and is a modest inhibitor of the remaining caspases.

MPT0B392 is an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation.