P450 (e.g. CYP17)

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1123	Abiraterone	0.02 mg/mL	0.1 mg/mL	0.2 mg/mL
S1185	Ritonavir	<1 mg/mL	100 mg/mL	3 mg/mL
S2246	Abiraterone Acetate	<1 mg/mL	<1 mg/mL	28 mg/mL
S1257	Posaconazole	<1 mg/mL	100 mg/mL	<1 mg/mL
S1442	Voriconazole	<1 mg/mL	70 mg/mL	20 mg/mL
S9257	Acetylshikonin	-1 mg/mL	2 mg/mL	-1 mg/mL
S9163	Rhapontigenin	-1 mg/mL	51 mg/mL	-1 mg/mL
S5380	7-Hydroxyflavone	-1 mg/mL	47 mg/mL	-1 mg/mL
S5266	Stiripentol	13 mg/mL	46 mg/mL	46 mg/mL
S5529	Galangin	<1 mg/mL	54 mg/mL	30 mg/mL
S4938	Cedrol	-1 mg/mL	44 mg/mL	-1 mg/mL
S2187	Avasimibe	<1 mg/mL	100 mg/mL	8 mg/mL
S1353	Ketoconazole	<1 mg/mL	5 mg/mL	7 mg/mL
S2476	Itraconazole	<1 mg/mL	7 mg/mL	<1 mg/mL
S1331	Fluconazole	<1 mg/mL	61 mg/mL	61 mg/mL
S1195	TAK-700 (Orteronel)	<1 mg/mL	61 mg/mL	8 mg/mL
S2803	Galeterone	<1 mg/mL	24 mg/mL	40 mg/mL
S2555	Clarithromycin	<1 mg/mL	25 mg/mL	<1 mg/mL
S2900	Cobicistat (GS-9350)	<1 mg/mL	100 mg/mL	100 mg/mL
S2496	Ozagrel	<1 mg/mL	46 mg/mL	<1 mg/mL
S1739	Thiabendazole	<1 mg/mL	40 mg/mL	1 mg/mL
S2046	Pioglitazone HCl	<1 mg/mL	79 mg/mL	4 mg/mL
S2067	Ozagrel HCl	52 mg/mL	52 mg/mL	6 mg/mL
S1952	Methoxsalen	<1 mg/mL	43 mg/mL	5 mg/mL
S2526	Alizarin	<1 mg/mL	48 mg/mL	<1 mg/mL
S2921	PF-4981517	<1 mg/mL	91 mg/mL	<1 mg/mL
S2043	Memantine HCl	30 mg/mL	43 mg/mL	43 mg/mL
S2380	Diosmetin	<1 mg/mL	60 mg/mL	<1 mg/mL
S2262	Apigenin	<1 mg/mL	54 mg/mL	<1 mg/mL
S2268	Baicalein	<1 mg/mL	54 mg/mL	<1 mg/mL
S2389	Naringin Dihydrochalcone	<1 mg/mL	100 mg/mL	100 mg/mL
S2394	Naringenin	<1 mg/mL	54 mg/mL	5 mg/mL
S3777	Gentiopicroside	-1 mg/mL	71 mg/mL	-1 mg/mL
S2401	Sodium Danshensu	2 mg/mL	7 mg/mL	<1 mg/mL
S3673	Sulfaphenazole	<1 mg/mL	62 mg/mL	62 mg/mL
S3660	Uniconazole	<1 mg/mL	58 mg/mL	58 mg/mL
S2329	Naringin	<1 mg/mL	100 mg/mL	2 mg/mL
S4221	Benzbromarone	<1 mg/mL	85 mg/mL	9 mg/mL
S2344	Piperine	<1 mg/mL	57 mg/mL	57 mg/mL
S1712	Deferasirox	<1 mg/mL	74 mg/mL	2 mg/mL
S4155	Chlorzoxazone	<1 mg/mL	34 mg/mL	34 mg/mL
S4741	Danshensu	23 mg/mL	<1 mg/mL	<1 mg/mL

Isoform-specific Inhibitors

P450 (e.g. CYP17) Inhibitors (43)
New P450 (e.g. CYP17) Products

Catalog No.	Information	Product Use Citations	Product Validations
S1123	Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay.	Nature, 2018, 560(7718):372-376 J Biol Chem, 2015, 290(6):3248-68 Chem Res Toxicol, 2012, 25(8):1720-31	A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.
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.	Blood, 2012, 119(20):4686-97 J Immunol, 2014, 192(8):3496-506 Antiviral Res, 2015, 120:140-6	(A) KMS11 and (B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown). (C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to untreated cells (not shown).
S2246	Abiraterone Acetate Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay.	Br J Cancer, 2018, 10.1038/s41416-018-0158-y J Biol Chem, 2015, 290(6):3248-68 Endocrinology, 2014, 155(2):358-69	Concomitant Western blot analysis of ER and TFF1 assessed after 16 h treatment with E2 or abiraterone in the presence or absence of MG-132 (10 μM).
S1257	Posaconazole Posaconazole 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.	Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother, 2015, 59(5):2654-65 Eur J Pharm Sci, 2016, 10.1016/j.ejps.2016.05.009	Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
S1442	Voriconazole Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.	Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother, 2015, 59(5):2654-65 Antimicrob Agents Chemother, 2015, 59(9):5548-54	Voriconazole increases the osteogenic activity of human osteoblasts in vitro. Osteoblasts were exposed to voriconazole (VCZ) or fluconazole (FCZ) at 15 or 200 μg/ml in osteoinductive medium (OS+) for up to 7 days. As a positive control, cells were also exposed to sodium fluoride (NaF) at 10 μM in nonosteoinductive medium (OS−). Osteoblastic differentiation was evaluated by measuring alkaline phosphatase (ALP) activity (A) and staining for calcium deposition with alazarin red S stain (B and C); calcium deposition was quantified by measuring the absorbance (A415) of extracted alazarin red S (B) and was assessed by the light microscopic appearance (white arrows) of stained osteoblast cultures (C). Values represent the means ± SD. *, P < 0.05, compared to osteoblasts grown under osteogenic conditions without treatment.
S9257^New	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.
S9163^New	Rhapontigenin Rhapontigenin, 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).
S5380^New	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.
S5266^New	Stiripentol Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S5529^New	Galangin Galangin, 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^New	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.
S4938^New	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.
S2187	Avasimibe Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.	Nature, 2016, 531(7596):651-5 Oncogene, 2016, 35(50):6378-6388 Nanomedicine, 2018, 14(8):2541-2550	a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11).
S1353	Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.	Cancer Manag Res, 2018, 10:4421-4438 Clin Cancer Res, 2017, 23(20):6203-6214
S2476	Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.	Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother, 2015, 59(9):5548-54 Med Mycol, 2016, 10.1093/mmy/myw131	Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies.
S1331	Fluconazole Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.	Antimicrob Agents Chemother, 2015, 59(4):2388-97 Int J Antimicrob Agents, 2017, 49(6):740-748 Int J Antimicrob Agents, 2017, 10.1016/j.ijantimicag.2017.01.029
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.	Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2803	Galeterone Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.	Biochem Biophys Res Commun, 2016, 477(4):1005-10 Steroids, 2018, 138:82-90	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S2555	Clarithromycin Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
S2900	Cobicistat (GS-9350) Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.	Antimicrob Agents Chem, 2017, 10.1128/AAC.01776-16	Effects of rifampin alone or in combination with cobicistat on the mean DRV CLint.app. in primary human hepatocytes in vitro. Cryopreserved primary human hepatocytes were incubated with RIF (0.5 to 20 μM) (hatched bars) or with COBI (0.13 to 12.76 μM) and RIF (0.5 to 20 μM) (gray bars) for 72 h. All cells were then incubated with RIF (0.5 to 20 M) or RIF (0.5 to 20 μM) together with COBI (0.13 to 12.76 μM), as described above, together with DRV (5 μM) for 60 min. Control cells were treated with DRV (5 μM) alone for 60 min (black bar). The results shown represent the mean DRV CLint.app. from three biological replicates measured in hepatocytes from three independent donors (donors HU1399, HU1574, and HU1587). Error bars indicate SDs.
S2496	Ozagrel Ozagrel is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S1739	Thiabendazole Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).
S2046	Pioglitazone HCl Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes.	Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2067	Ozagrel HCl Ozagrel HCl is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S1952	Methoxsalen Methoxsalen is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.
S2526	Alizarin Alizarin 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.
S2921	PF-4981517 PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
S2043	Memantine HCl Memantine HCl is a CYP2B6 and CYP2D6 inhibitor for recombinant CYP2B6 and CYP2D6 with K_i of 0.51 nM and 94.9 μM, respectively.
S2380	Diosmetin Diosmetin is a bioflavonoid found in spearmint, oregano, and many other plants.
S2262	Apigenin Apigenin is a potent P450 inhibitor for CYP2C9 with K_i of 2 μM.	Oncol Rep, 2015, 34(4):1805-14 Int J Clin Exp Pathol, 2014, 7(7):3938-3947 Oxid Med Cell Longev, 2017, 2017:4397340	The effects of apigenin and GLUT-1 AS-ODNs on xenograft apoptosis (the second experiment), observed an under optical microscope (magnification, ×400), and the percentage of apoptotic cells in 100 cells per field was counted and used to calculate the mean apoptosis index (AI). AI, apoptotic index.
S2268	Baicalein Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.	J Nutr Biochem, 2013, 24(11):1953-62 Mol Cell Biochem, 2015, 10.1007/s11010-015-2429-8 Biochem Biophys Res Commun, 2016, 473(4):775-80	Baicalein suppresses the viability of DU 145 and PC-3 cells. b DU145 cells and c PC-3 cells were treated with different concentrations of baicalein for 24, 48, and 72 h. Baicalein significantly inhibited the viability of both cell lines in a dose-and time-dependent manner. The results are presented as the means ± SD of three independent experiments and the corresponding standard error. P<0.05; *P<0.01.
S2389	Naringin Dihydrochalcone Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes.
S2394	Naringenin Naringenin is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.	Sci Rep, 2016, 6:27268	(d) Antiviral activity of SZA on assembly and release. Huh7 cells were electroporated with JFH-1 RNA of HCV, followed by 4 h treatment of the indicated concentrations of SZA. At 48 h after electroporation, cells were subjected to three cycles of freeze and thaw to test the intracellular viral infectivity; supernatants of the electroporated cells were collected for the detection of extracellular viral infectivity. 100 μM naringenin was introduced as a positive control. Results are shown as relative HCV infectivity compared to DMSO treated group. Data shown as mean ± SD of three independent experiments.
S3777	Gentiopicroside Gentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S2401	Sodium Danshensu Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.
S3673	Sulfaphenazole Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
S3660	Uniconazole Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis.
S2329	Naringin Naringin is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.
S4221	Benzbromarone Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with K_i value of 19.3 nM.
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.	Int J Mol Med, 2015, 36(5):1369-76	Piperine attenuates inflammation in the substantia nigra (SN) of the MPTP-treated brains. (A) Iba-1-immunostaining was performed on brain sections for microglia. Piperine alleviated microglia activating caused by MPTP. (B) Brain tissue was stained with the anti-interleukin-1β (IL-1β) antibody in the SN. MPTP notably increased the expression of IL-1β in the SN of the mice and the increase was partly blocked by piperine. (C) Western blot analysis of IL-1β expression in the SN. (D) Densitometric analysis of western blot analyses of IL-1β. Densitometry was measured by Quantity One 1-D analyze software (Universal Hood II; Bio-Rad Laboratories, Hercules, CA, USA). Values are presented as mean ± standard deviation, *P<0.05, compared to MPTP.
S1712	Deferasirox Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.	Nature, 2014, 509(7498):105-9	U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox.
S4155	Chlorzoxazone Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.
S4741	Danshensu Danshensu, a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects.

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Isoform-specific Inhibitors