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.

Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor.

Liarozole (R75251; R85246) is an imidazole derivative and a retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.

Liarozole 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.

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively.

Ticlopidine (PCR 5332), an antithrombotic prodrug, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 µM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 µM and 149 µM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.

Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier.

Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.

CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin.

8-BOA is a selective and potent mechanism-based inactivator of breast cancer-associated CYP4Z1.8-BOA exhibited favourable inhibitory activity in vitro, thus meriting in vivo characterization.

DX-308 is a potent, selective dual CYP26A1/B1 inhibitor and retinoic acid metabolism blocking agent.DX308 does not interact with off‐target nuclear receptors or CYP450s, is not genotoxic, and is stable in skin, despite vigorous hepatic metabolism.Topical DX308 induces comedolysis and epidermal thickening without apparent adverse effects in vivo.DX308 shows potent modulation of retinoid‐responsive genes by DX308 in both healthy and keratinization disorder keratinocytes (KCs).DX 308 may present an improved therapeutic alternative for the treatment of keratinization disorders and other retinoid‐responsive skin ailments.

DX314 is a potent, specific CYP26B1 inhibitor with IC50 of 108 nM, >15-fold selectivity over CYP26A1.DX314 potentiates all-trans-RA (atRA) gene expression effects in healthy and diseased reconstructed human epidermis (RHE).DX314 potentiates the effects of atRA on the expression and localization of keratin 10 (KRT10), protects barrier function in RHE.DX314 reduces comedonal number, induces epidermal thickening, and increases comedonal profile, while having no effect on transepidermal water loss (TEWL) in treated rhino mice.

MEHP (Phthalic acid mono-2-ethylexyl ester) is a competitive inhibitor of CYP2C9 with IC50 of 6.37 μM.

BMS-737 (BMS737) is a potent, , selective, non-steroidal, reversible inhibitor of CYP17 lyase, 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase.

DLCI-1 is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

DLCI-1 dihydrochloride is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

ODM-208 (ODM208) is a potent, selective, orally bioavailable CYP11A1 inhibitor, inhibits the biosynthesis of pregnenolone with IC50 of 15 nM in NCI-H295R cells.

ODM-209 (ODM209) is a potent, selective, orally bioavailable inhibitor of CYP11A1 (cholesterol side-chain cleavage enzyme) with potential antineoplastic activity, inhibits the biosynthesis of pregnenolone.

TPP-IOA is a specific inhibitor of cytochrome c (cyt c) peroxidase activity, inhibits peroxidase activity of cardiolipin-induced cytochrome c peroxidase activity with IC50 of 5 uM.