P450 (e.g. CYP17)
Inhibitory Selectivity
Isoform-specific Inhibitors
P450 (e.g. CYP17) Products
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S2526 |
AlizarinAlizarin (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-Dihydroxyanthraquinone2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity. |
||
S0721 |
TiclopidineTiclopidine (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-4981517PF-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 |
HypericinHypericin (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). |
||
S3291 |
MyristicinMyristicin (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 hydrochlorideDazoxiben 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 |
IsosilybinIsosilybin (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 |
AcetylshikoninAcetylshikonin 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 F1Ginsenoside 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 |
PurpurinPurpurin (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 |
APD597APD-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 |
CurcumenolCurcumenol, 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 |
DMU2105DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM. |
||
S0176 |
DMU2139DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM. |
||
S6886 |
1-Aminobenzotriazole1-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 |
BergaptolBergaptol (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-Hydroxyflavone7-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 |
GalanginGalangin (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. |
||
S5429 |
Diallyl sulfideDiallyl 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 IIIPolygalaxanthone 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. |
||
S6594 |
Liarozole dihydrochlorideLiarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively. |
||
S9163 |
RhapontigeninRhapontigenin (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-400NVP-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-Dimethoxyflavone5,7-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. |
||
S6437 |
Oxolamine CitrateOxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect. |
||
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) mesylateAlflutinib (AST2818, Furmonertinib) 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. |
||
S5967 |
Berberine chloride hydrateBerberine (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. |
||
S4784 |
PhloracetophenonePhloracetophenone, 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. |
||
S6606 |
CDD3505CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. |
||
S5969 |
Dicloxacillin Sodium hydrateDicloxacillin 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. |
||
S6790 |
Ellipticine hydrochlorideEllipticine 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 |
AlizarinAlizarin (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-Dihydroxyanthraquinone2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity. |
||
S0721 |
TiclopidineTiclopidine (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-4981517PF-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 |
HypericinHypericin (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). |
||
S3291 |
MyristicinMyristicin (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 hydrochlorideDazoxiben 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 |
IsosilybinIsosilybin (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 |
AcetylshikoninAcetylshikonin 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 F1Ginsenoside 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 |
PurpurinPurpurin (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 |
APD597APD-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 |
CurcumenolCurcumenol, 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 |
DMU2105DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM. |
||
S0176 |
DMU2139DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM. |
||
S6886 |
1-Aminobenzotriazole1-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 |
BergaptolBergaptol (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-Hydroxyflavone7-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 |
GalanginGalangin (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. |
||
S5429 |
Diallyl sulfideDiallyl 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 IIIPolygalaxanthone 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. |
||
S6594 |
Liarozole dihydrochlorideLiarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively. |
||
S9163 |
RhapontigeninRhapontigenin (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-400NVP-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-Dimethoxyflavone5,7-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. |
||
S6437 |
Oxolamine CitrateOxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect. |
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) mesylateAlflutinib (AST2818, Furmonertinib) 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. |
||
S5967 |
Berberine chloride hydrateBerberine (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. |
||
S4784 |
PhloracetophenonePhloracetophenone, 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 |
---|---|---|---|
S6606 |
CDD3505CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. |
||
S5969 |
Dicloxacillin Sodium hydrateDicloxacillin 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. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S6790 |
Ellipticine hydrochlorideEllipticine 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. |