P450 (e.g. CYP17)

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1123 Abiraterone 0.02 mg/mL 0.1 mg/mL 0.2 mg/mL
S1185 Ritonavir <1 mg/mL 100 mg/mL 3 mg/mL
S2246 Abiraterone Acetate <1 mg/mL <1 mg/mL 28 mg/mL
S1257 Posaconazole <1 mg/mL 100 mg/mL <1 mg/mL
S1442 Voriconazole <1 mg/mL 70 mg/mL 20 mg/mL
S4741 Danshensu 23 mg/mL <1 mg/mL <1 mg/mL
S1712 Deferasirox <1 mg/mL 74 mg/mL 2 mg/mL
S2187 Avasimibe <1 mg/mL 100 mg/mL 8 mg/mL
S1353 Ketoconazole <1 mg/mL 5 mg/mL 7 mg/mL
S2476 Itraconazole <1 mg/mL 7 mg/mL <1 mg/mL
S1331 Fluconazole <1 mg/mL 61 mg/mL 61 mg/mL
S1195 TAK-700 (Orteronel) <1 mg/mL 61 mg/mL 8 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S2555 Clarithromycin <1 mg/mL 25 mg/mL <1 mg/mL
S2900 Cobicistat (GS-9350) <1 mg/mL 100 mg/mL 100 mg/mL
S2496 Ozagrel <1 mg/mL 46 mg/mL <1 mg/mL
S1739 Thiabendazole <1 mg/mL 40 mg/mL 1 mg/mL
S2046 Pioglitazone HCl <1 mg/mL 79 mg/mL 4 mg/mL
S2067 Ozagrel HCl 52 mg/mL 52 mg/mL 6 mg/mL
S1952 Methoxsalen <1 mg/mL 43 mg/mL 5 mg/mL
S2526 Alizarin <1 mg/mL 48 mg/mL <1 mg/mL
S4155 Chlorzoxazone <1 mg/mL 34 mg/mL 34 mg/mL
S2921 PF-4981517 <1 mg/mL 91 mg/mL <1 mg/mL
S2380 Diosmetin <1 mg/mL 60 mg/mL <1 mg/mL
S2262 Apigenin <1 mg/mL 54 mg/mL <1 mg/mL
S2268 Baicalein <1 mg/mL 54 mg/mL <1 mg/mL
S2394 Naringenin <1 mg/mL 54 mg/mL 5 mg/mL
S2401 Sodium Danshensu 2 mg/mL 7 mg/mL <1 mg/mL
S2329 Naringin <1 mg/mL 100 mg/mL 2 mg/mL
S4221 Benzbromarone <1 mg/mL 85 mg/mL 9 mg/mL
S2344 Piperine <1 mg/mL 57 mg/mL 57 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1123

Abiraterone

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

S1185

Ritonavir

Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases.

S2246

Abiraterone Acetate

Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

S1257

Posaconazole

Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

S1442

Voriconazole

Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

S2187

Avasimibe

Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.

S1353

Ketoconazole

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

S2476

Itraconazole

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.

S1331

Fluconazole

Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

S1195

TAK-700 (Orteronel)

TAK-700 (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.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S2555

Clarithromycin

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

S2900

Cobicistat (GS-9350)

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

S2496

Ozagrel

Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1739

Thiabendazole

Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).

S2046

Pioglitazone HCl

Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.

S2067

Ozagrel HCl

Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1952

Methoxsalen

Methoxsalen is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.

S2526

Alizarin

Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

S2921

PF-4981517

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S2380

Diosmetin

Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.

S2262

Apigenin

Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

S2268

Baicalein

Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.

S2394

Naringenin

Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.

S2401

Sodium Danshensu

Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.

S2329

Naringin

Naringin is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.

S4221

Benzbromarone

Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.

S2344

Piperine

Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.

S4741New

Danshensu

Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects.

S1712

Deferasirox

Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

S4155

Chlorzoxazone

Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.

Catalog No. Information Product Use Citations Product Validations
S1123

Abiraterone

Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.

S1185

Ritonavir

Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases.

S2246

Abiraterone Acetate

Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.

S1257

Posaconazole

Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

S1442

Voriconazole

Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

S2187

Avasimibe

Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.

S1353

Ketoconazole

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

S2476

Itraconazole

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.

S1331

Fluconazole

Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

S1195

TAK-700 (Orteronel)

TAK-700 (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.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S2555

Clarithromycin

Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

S2900

Cobicistat (GS-9350)

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

S2496

Ozagrel

Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1739

Thiabendazole

Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).

S2046

Pioglitazone HCl

Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.

S2067

Ozagrel HCl

Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

S1952

Methoxsalen

Methoxsalen is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.

S2526

Alizarin

Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

S2921

PF-4981517

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S2380

Diosmetin

Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.

S2262

Apigenin

Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.

S2268

Baicalein

Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.

S2394

Naringenin

Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.

S2401

Sodium Danshensu

Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.

S2329

Naringin

Naringin is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.

S4221

Benzbromarone

Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.

S2344

Piperine

Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.

Catalog No. Information Product Use Citations Product Validations
S4741New

Danshensu

Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects.

S1712

Deferasirox

Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

2014, 509(7498):105-9

S4155

Chlorzoxazone

Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.