Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.

Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.

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

CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

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

DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10, 742 nM for CYP1B1 and CYP1A1, respectively.

DMU-2105(CYP1B1 inhibitor 7k) is a potent and specific CYP1B1 inhibitor.

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).

HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.

Methoxsalen (Oxsoralen)

TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM.

TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC).

CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM.

Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia.

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).

Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM. Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM). Kushenol K also inhibits the activity of SGLT1 and SGLT2.

Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki=68 nM), a family of enzymes that catabolize Abscisic acid, and thus, suppress gibberellin and sterol biosynthesis.

Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.

7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase.

β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.

Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP), with IC50 values of 1.29 μM for CYP3A4 in in human liver microsomes.

2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.