P450 (e.g. CYP17)

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.

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 a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM.

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, 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.

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.

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.

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.

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 a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM.

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, 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.

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.

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.