cyp17

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.

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.

CYP17A1-IN-1 (Compound 14) is an inhibitor of CYP17A1 with an IC50 of 26 nM. It exhibits cytotoxicity in androgen-sensitive prostate cancer cells, specifically LNCaP, and hinders the migration of DU-145 cells.

EN3356 is an orally available and selective inhibitor of steroidal 17-alpha-hydroxylase C17,20 cleavage enzyme (CYP17A1 or CYP17), a non-steroidal cleavage enzyme-selective compound with potential anti-androgenic and anti-tumor activity.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

Seviteronel racemate is the racemate form of Seviteronel and is a potent inhibitor of CYP17 lyase.

Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1 AMP-activated protein kinase peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.

Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.

Abiraterone decanoate is a prodrug of Abiraterone that provides controlled release and long-lasting CYP17 inhibition of Abiraterone using intramuscular (IM) delivery.

Hypaconitine, an active and highly toxic constituent derived from Aconitum species, possesses anti-inflammatory activity and is widely used to treat rheumatism.

CFG920 is a CYP17 inhibitor, is also an orally available inhibitor of the steroid 17-alpha-hydroxylase C17,20 lyase (CYP17A1 or CYP17), with potential antiandrogen and antineoplastic activities. Upon oral administration, CYP17 inhibitor CFG920 inhibits the enzymatic activity of CYP17A1 in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.

15-Hydroxydehydroabietic acid exhibits a promising alpha-glucosidase inhibitory activity, it also shows significant antibacterial activities.

β-Sparteine is a class 1a antiarrhythmic agent, a sodium channel blocker. The deficient debrisoquine hydroxylation of Sparteine is due to the absence of P-450IID1 protein in the livers of poor metabolizers.