caspase-4

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.

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

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

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.

ML132 is an effective and selective inhibitor of caspase 1 (IC50: 0.316 nM).

VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective, and blood-brain barrier permeable inhibitor of the interleukin-converting enzyme/caspase-1 subfamily caspases, displaying Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4, respectively.

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

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

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.

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.

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Diclofenac Diethylamine, a non-selective COX inhibitor, is utilized as a nonsteroidal anti-inflammatory drug (NSAID).

Diclofenac sodium (GP 45840) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

4-Vinylcyclohexene Dioxide (VCD) is an industrial epoxy resin intermediate and metabolite that exhibits a highly selective destructive effect on oocytes in primordial and primary follicles; it is used as a key inducer for establishing animal models of premature ovarian failure and premenopause. 4-Vinylcyclohexene Dioxide exerts its ovarian toxicity by activating caspase-dependent apoptotic pathways and can induce apoptosis in ovarian granulosa cells by upregulating reactive oxygen species and activating the PI3K/Akt/mTOR signaling pathway. It is used in reproductive toxicology and endocrine regulation research.

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg/L.3 ALPHA-PINENE (100 μg/ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16/F10 melanoma cells [4]. In a B16/F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg/ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg/L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

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.

CGP74514A is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor with an IC50 of 25 nM. It effectively inhibits the activity of the CDK1/cyclin B complex, arrests the cell cycle at G2/M phase, and further induces apoptosis in tumor cells, showing promising application prospects in bladder cancer research.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

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.

Talampanel (LY-300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor antagonist with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models.

Ac-DEVD-AMC (AC-ASP-MET-GLN-ASP-7-AMINO-4-METHYLCOUMARIN) is the substrate of Caspase-3 .

GQN-B37-Me is an MCL-1 inhibitor that can induce caspase-dependent apoptosis. It exhibits significant cytotoxicity in H929 (IC50= 3.71 μM) and MV-4-11 (IC50= 5.57 μM) cell lines. GQN-B37-Me is useful for leukemia research.

VEGFR-2-IN-69 (Compound 5A) is an inhibitor of VEGFR-2 and telomerase (Telomerase) that enhances the expression of caspase 3, caspase 8, and caspase 9, while reducing the levels of CDK-2, CDK-4, and CDK-6. It has an IC50 of 15.46 µM against HCT116.