CYP3 Selective Inhibitors | Activators

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S2476	Itraconazole (R 51211)	Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.	Selective	CYP3A4, IC50: 6.1 nM
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.	Selective	CYP3A4, IC50: 30 nM
S2900	Cobicistat	Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.	Selective	CYP3A, IC50: 30 nM-285 nM
S6868	Alflutinib (AST2818) mesylate	Alflutinib (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.	Selective	CYP3A4, EC50: 0.25 μM
S3766	Tanshinone IIA sulfonate sodium	Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE)	Selective	CYP3A4, IC50: 6.377 μM
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.	Selective	CYP3A4, IC50: 12.6 μM
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.	Selective	CYP3A4, IC50: 24.92 μM
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.	Selective	CYP3A4, Ki: 67.8 μM
S9250	Isosilybin	Isosilybin (Silymarin, 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.	Selective	CYP3A4, IC50: 74 μM
S1257	Posaconazole (SCH 56592)	Posaconazole (SCH 56592,POS,Noxafil) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.	Selective
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.	Selective
S2555	Clarithromycin	Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.	Selective
S1185	Ritonavir	Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.	Selective
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.	Selective
S4938	Cedrol	Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.	Pan	CYP3A4, Ki: 3.4 μM
S2046	Pioglitazone HCl	Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent	Pan	CYP3A4, Ki: 11.8 μM
S3931	Ginsenoside Rd	Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP	Pan	CYP3A4, IC50: 81.7 μM