cyp 17

CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.

Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.

Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.

Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).

Phthalic acid mono-2-ethylhexyl ester (Phthalic Acid Monooctyl Ester) is a major bioactive metabolite of diethylhexyl phthalate (DEHP), which inhibits the 17,20 lyase activity of CYP17. The Cyp17a1 gene is specifically targeted by MEHP, explaining the MEHP-induced suppression of steroidogenesis observed.

Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblasts in osteoporotic patients. Actein's ability to pathways involved in lipid disorders and carci

Myristicin (Myristicine) is a natural product found in spices and umbelliferous plants. Myristicin has anti-cholinergic, Antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytokines,chemokines, and growth factors in dsRNA-stimulated macrophages via the calcium pathway. Myristicin can induce Apoptosis as characterised by alterations in the mitochondrial membrane potential, cytochrome c release, Caspase-3 activation, PARP-cleavage and DNA fragmentation.

Vasicinone may act as a hepatoprotective agent. (±)-Vasicinone has significant antitussive, expectorant, and bronchodilating activities, which can be used to treat respiratory disease.(S)-Vasicinone exhibits antiproliferative activity against human gastric cancer cells MCG-803.

(S)-(-)-Canadine (tetrahydroberberine) is a naturally occurring isoquinoline alkaloid, acting as a D2 receptor antagonist and 5-HT1A receptor agonist, capable of blocking dopamine-stimulated adenylate cyclase activity. (S)-(-)-Canadine also enhances gastrointestinal motility, blocks K(ATP) channels in substantia nigra pars compacta (SNc) dopaminergic neurons, and exerts neuroprotective effects.

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg/mL.

Isocupressic acid ((+)-Isocupressic acid) is an abortifacient isolated from pine needles and bark that blocks progesterone production in bovine corpus luteum cells.

Lecanoric acid is a compound derived from Lecanoric acid, which has antioxidant activity and promotes the growth of probiotics.

Licopyranocoumarin could as a potent neuroprotective drug via markedly blocked MPP+-induced neuronal PC12D cell death and disappearance of mitochondrial membrane potential, which were mediated by JNK.

Zederone is a natural sesquiterpene that modulates inflammatory response, smooth muscle relaxation and endocrinology to treat dysmenorrhea; down-regulates mRNA levels of mTOR and p70s6K to inhibit the proliferation of ovarian cancer cells, and interacts with hypoglycemic proteins 3L4Y and 5UBA to be anti-diabetic and anti-oxidant.

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

TAK-700 salt is a potent and highly selective inhibitor of human 17,20-lyase with an IC50 of 38 nM and is over 1000-fold more selective than other CYPs such as 11-hydroxylase and CYP3A4.

TAK-700 (Orteronel) (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.

CYP4A11/CYP4F2-IN-1 is a cytochrome P450 (CYP) 4A11 and CYP4F2 inhibitor, applicable for research on kidney, cardiovascular, and cerebrovascular diseases.

(±)17(18)-EpETE-Ethanolamide, an ω-3 endocannabinoid epoxide, originates from eicosapentaenoic ethanolamide (EPEA) through cytochrome P450 (CYP) epoxygenases action and is decomposed by soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FA, AH). Its endogenous synthesis occurs in LPS-stimulated and EPEA-supplemented BV-2 microglia cells, a process inhibited by the CYP inhibitor ketoconazole. This compound mitigates IL-6 and nitrite levels while enhancing IL-10 production following LPS exposure in BV-2 microglia. At a dose of 50 µM, it prevents platelet aggregation caused by arachidonic acid but not that triggered by ADP, collagen, or ristocetin. Additionally, it facilitates the dilation of constricted bovine coronary arteries (ED50= 1.1 µM) and blocks VEGF-driven tubulogenesis in human microvascular endothelial cells (HMVECs).