P450 (e.g. CYP17)

Inhibitory Selectivity

Isoform-specific Inhibitors

P450 (e.g. CYP17) Products

New P450 (e.g. CYP17) Products
Catalog No. Information Product Use Citations Product Validations
S2526

Alizarin

Alizarin (Anthraquinonic) 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.

S5169

2,6-Dihydroxyanthraquinone

2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.

S0721

Ticlopidine

Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.

S2921

PF-4981517

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S3273

Hypericin

Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).

S5967New

Berberine chloride hydrate

Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6437New

Oxolamine Citrate

Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.

S3291

Myristicin

Myristicin (Myristicine), a terpene-like active component in Nutmeg which is the seed of Myristica fragrans, is a weak inhibitor of monamine oxidase (MAO) and a mechanism-based inhibitor of CYP1A2.

S0541

Dazoxiben hydrochloride

Dazoxiben hydrochloride (HCl) is a potent, selevtive and orally active inhibitor of thromboxane (TX) synthase. Dazoxiben inhibits TXB2 production in clotting human whole blood with IC50 of 0.3 μM and causes parallel enhancement of PGE2 production.

S9250

Isosilybin

Isosilybin (Silymarin, Silybin B, Isosilybinin, Q-100795) is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.

S9257

Acetylshikonin

Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.

S9299

Ginsenoside F1

Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.

S4963

Purpurin

Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin) is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities. Purpurin strongly inhibits the activities of CYP1A1, CYP1A2 and CYP1B1.

S0110

APD597

APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).

S3874

Curcumenol

Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.

S3660

Uniconazole (S 3307D)

Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.

S0175

DMU2105

DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM.

S0176

DMU2139

DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM.

S6886

1-Aminobenzotriazole

1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).

S9442

Bergaptol

Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin) is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.

S5380

7-Hydroxyflavone

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.

S5529

Galangin

Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.

S2274

TMS

TMS is a potent, selective and competitive cytochrome P450 1B1 (CYP1B1) inhibitor with IC50 of 6 nM. TMS exhibits 50-fold selectivity for P450 1B1 over P450 1A1 with IC50 of 300 nM and 500-fold over P450 1A2 with IC50 of 3 μM.

S5429

Diallyl sulfide

Diallyl sulfide, a thioether found naturally in garlic, is a selective inhibitor and also a substrate of CYP2E1 with an IC50 of 17.3 μM. It has protective effects against alcohol- and acetaminophen-induced hepatotoxicity in many studies.

S9241

Polygalaxanthone III

Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.

S9163

Rhapontigenin

Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).

S0230

NVP-VID-400

NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.

S3227

5,7-Dimethoxyflavone

5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP, ABCG2) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.

S2271

Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.

S4784

Phloracetophenone

Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae). Phloracetophenone can stimulate CYP7A1 activity. Phloracetophenone induces cholestasis in rats mediated through Mrp2.

S5969New

Dicloxacillin Sodium hydrate

Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil), a narrow-spectrum β-Lactam antibiotic of the penicillin class, induces drug-metabolizing CYP enzymes to a clinically relevant extent.

S6606

CDD3505

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

S6790

Ellipticine hydrochloride

Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.

Catalog No. Information Product Use Citations Product Validations
S2526

Alizarin

Alizarin (Anthraquinonic) 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.

S5169

2,6-Dihydroxyanthraquinone

2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.

S0721

Ticlopidine

Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.

S2921

PF-4981517

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

S3273

Hypericin

Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).

S5967New

Berberine chloride hydrate

Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6437New

Oxolamine Citrate

Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.

S3291

Myristicin

Myristicin (Myristicine), a terpene-like active component in Nutmeg which is the seed of Myristica fragrans, is a weak inhibitor of monamine oxidase (MAO) and a mechanism-based inhibitor of CYP1A2.

S0541

Dazoxiben hydrochloride

Dazoxiben hydrochloride (HCl) is a potent, selevtive and orally active inhibitor of thromboxane (TX) synthase. Dazoxiben inhibits TXB2 production in clotting human whole blood with IC50 of 0.3 μM and causes parallel enhancement of PGE2 production.

S9250

Isosilybin

Isosilybin (Silymarin, Silybin B, Isosilybinin, Q-100795) is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.

S9257

Acetylshikonin

Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.

S9299

Ginsenoside F1

Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.

S4963

Purpurin

Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin) is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities. Purpurin strongly inhibits the activities of CYP1A1, CYP1A2 and CYP1B1.

S0110

APD597

APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).

S3874

Curcumenol

Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.

S3660

Uniconazole (S 3307D)

Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.

S0175

DMU2105

DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM.

S0176

DMU2139

DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM.

S6886

1-Aminobenzotriazole

1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).

S9442

Bergaptol

Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin) is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.

S5380

7-Hydroxyflavone

7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.

S5529

Galangin

Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.

S2274

TMS

TMS is a potent, selective and competitive cytochrome P450 1B1 (CYP1B1) inhibitor with IC50 of 6 nM. TMS exhibits 50-fold selectivity for P450 1B1 over P450 1A1 with IC50 of 300 nM and 500-fold over P450 1A2 with IC50 of 3 μM.

S5429

Diallyl sulfide

Diallyl sulfide, a thioether found naturally in garlic, is a selective inhibitor and also a substrate of CYP2E1 with an IC50 of 17.3 μM. It has protective effects against alcohol- and acetaminophen-induced hepatotoxicity in many studies.

S9241

Polygalaxanthone III

Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.

S9163

Rhapontigenin

Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).

S0230

NVP-VID-400

NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.

S3227

5,7-Dimethoxyflavone

5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP, ABCG2) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.

Catalog No. Information Product Use Citations Product Validations
S2271

Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.

S4784

Phloracetophenone

Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae). Phloracetophenone can stimulate CYP7A1 activity. Phloracetophenone induces cholestasis in rats mediated through Mrp2.

Catalog No. Information Product Use Citations Product Validations
S5969New

Dicloxacillin Sodium hydrate

Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil), a narrow-spectrum β-Lactam antibiotic of the penicillin class, induces drug-metabolizing CYP enzymes to a clinically relevant extent.

S6606

CDD3505

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

Catalog No. Information Product Use Citations Product Validations
S6790

Ellipticine hydrochloride

Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.