P450 (e.g. CYP17)
Isoform-specific Inhibitors
P450 (e.g. CYP17) Products
Catalog No. | Information | Product Use Citations | Product Validations |
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S1123 |
AbirateroneAbiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor. |
![]() ![]() Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
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S1185 |
RitonavirRitonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) 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. |
![]() ![]() (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).
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S2246 |
Abiraterone AcetateAbiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor. |
![]() ![]() BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. *, P < .05; **, P < .01; ***, P < .005; ****, P < .001.
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S1257 |
PosaconazolePosaconazole (SCH56592) 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. |
![]() ![]() 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.
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S6437New |
Oxolamine CitrateOxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect. |
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S3273New |
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). |
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S3291New |
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. |
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S6886New |
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). |
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S3227New |
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. |
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S6868New |
Alflutinib (AST2818) mesylateAlflutinib (AST2818) 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. |
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S0721New |
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. |
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S0541New |
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. |
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S0230New |
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. |
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S0175New |
DMU2105DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM. |
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S0176New |
DMU2139DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM. |
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S2187 |
AvasimibeAvasimibe (CI-1011, PD-148515) 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. |
![]() ![]() 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). |
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S1353 |
KetoconazoleKetoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor. |
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S2476 |
ItraconazoleItraconazole (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. |
![]() ![]() 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. |
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S1331 |
FluconazoleFluconazole (UK 49858) 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. |
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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). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3. |
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S2803 |
GaleteroneGaleterone (TOK-001) 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. |
![]() ![]() 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. |
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S4202 |
Verapamil HClVerapamil HCl (CP-16533-1) is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4. |
![]() ![]() The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
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S2555 |
ClarithromycinClarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections. |
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S2900 |
Cobicistat (GS-9350)Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM. |
![]() ![]() 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.
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S2496 |
OzagrelOzagrel (OKY-046) 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. |
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S1739 |
ThiabendazoleThiabendazole 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). |
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S2046 |
Pioglitazone HClPioglitazone 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 ferroptosis. |
![]() ![]() 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. |
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S2067 |
Ozagrel HClOzagrel HCl (OKY-046) is a selective |
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S1952 |
MethoxsalenMethoxsalen (Xanthotoxin, NCI-C55903) 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. |
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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. |
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S1794 |
FenofibrateFenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy. |
![]() ![]() E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
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S5169 |
2,6-Dihydroxyanthraquinone2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity. |
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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. |
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S5266 |
StiripentolStiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450. |
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S5252 |
Ozagrel sodiumOzagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties. |
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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. |
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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. |
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S5658 |
Omeprazole SodiumOmeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19. |
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S7456 |
Osilodrostat (LCI699)LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis. |
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S2380 |
DiosmetinDiosmetin (Luteolin 4-methyl ether) is a bioflavonoid found in spearmint, oregano, and many other plants. |
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S2262 |
ApigeninApigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM. |
![]() ![]() Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration. |
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S4938 |
CedrolCedrol, 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. |
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S2268 |
BaicaleinBaicalein is a CYP2C9 and prolyl endopeptidase inhibitor. |
![]() ![]() 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. |
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S2389 |
Naringin DihydrochalconeNaringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes. |
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S5416 |
MetyraponeMetyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis. |
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S2394 |
NaringeninNaringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol) 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. |
![]() ![]() (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.
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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. |
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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. |
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S3777 |
GentiopicrosideGentiopicroside (GE, Gentiopicrin), 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. |
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S2401 |
Sodium DanshensuSodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza. |
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S3931 |
Ginsenoside RdGinsenoside 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, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
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S4831 |
Piperonyl butoxidePiperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.Piperonyl butoxide is an inhibitor of cytochrome P450 monooxygenases(P450s). |
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S3673 |
SulfaphenazoleSulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) 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). |
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S3766 |
Tanshinone IIA sulfonate sodiumSodium 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) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). |
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S3917 |
TetrahydrocurcuminTetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4. |
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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. |
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S3660 |
UniconazoleUniconazole (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. |
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S2329 |
NaringinNaringin (Naringoside) 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. |
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S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein. |
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S4221 |
BenzbromaroneBenzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM. |
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S3719 |
TopiroxostatTopiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment. |
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S2344 |
PiperinePiperine (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. |
![]() ![]() 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.
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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. |
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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. |
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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. |
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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. |
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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). |
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S2271 |
Berberine chlorideBerberine chloride (Natural Yellow 18 chloride) 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. |
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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. |
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S0110New |
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). |
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S6606 |
CDD3505CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. |
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S1442 |
VoriconazoleVoriconazole (UK-109496) 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. |
![]() ![]() 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. |
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S6790New |
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. |
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S1712 |
DeferasiroxDeferasirox (CGP-72670, ICL-670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death. |
![]() ![]() 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. |
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S4155 |
ChlorzoxazoneChlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1. |
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S4741 |
DanshensuDanshensu (Salvianic acid A), a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Danshensu inhibits CYP2E1 and CYP2C9 with IC50 of 36.63 and 75.76 μm, respectively. |
Catalog No. | Information | Product Use Citations | Product Validations |
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S1123 |
AbirateroneAbiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor. |
![]() ![]() Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
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S1185 |
RitonavirRitonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) 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. |
![]() ![]() (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).
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S2246 |
Abiraterone AcetateAbiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor. |
![]() ![]() BCaPT10 and BPH-1 cells were treated with vehicle (NTC, white bars), 10 uM abiraterone (ABI, gray bars), or abiraterone plus steroid hormones (black bars, 100 nM DHT, 10 nM estradiol, and 10 nM progestin). Minimum of 200 cells per condition was used from each of at least 3 independent experiments. Each result is shown as the average 盨EM from at least 3 independent experiments. One-way ANOVA. *, P < .05; **, P < .01; ***, P < .005; ****, P < .001.
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S1257 |
PosaconazolePosaconazole (SCH56592) 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. |
![]() ![]() 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.
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S6437New |
Oxolamine CitrateOxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect. |
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S3273New |
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). |
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S3291New |
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. |
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S6886New |
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). |
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S3227New |
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. |
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S6868New |
Alflutinib (AST2818) mesylateAlflutinib (AST2818) 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. |
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S0721New |
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. |
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S0541New |
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. |
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S0230New |
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. |
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S0175New |
DMU2105DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM. |
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S0176New |
DMU2139DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM. |
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S2187 |
AvasimibeAvasimibe (CI-1011, PD-148515) 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. |
![]() ![]() 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). |
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S1353 |
KetoconazoleKetoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor. |
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S2476 |
ItraconazoleItraconazole (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. |
![]() ![]() 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. |
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S1331 |
FluconazoleFluconazole (UK 49858) 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. |
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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). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3. |
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S2803 |
GaleteroneGaleterone (TOK-001) 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. |
![]() ![]() 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. |
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S4202 |
Verapamil HClVerapamil HCl (CP-16533-1) is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4. |
![]() ![]() The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
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S2555 |
ClarithromycinClarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections. |
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S2900 |
Cobicistat (GS-9350)Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM. |
![]() ![]() 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.
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S2496 |
OzagrelOzagrel (OKY-046) 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. |
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S1739 |
ThiabendazoleThiabendazole 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). |
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S2046 |
Pioglitazone HClPioglitazone 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 ferroptosis. |
![]() ![]() 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. |
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S2067 |
Ozagrel HClOzagrel HCl (OKY-046) is a selective |
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S1952 |
MethoxsalenMethoxsalen (Xanthotoxin, NCI-C55903) 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. |
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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. |
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S1794 |
FenofibrateFenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy. |
![]() ![]() E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
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S5169 |
2,6-Dihydroxyanthraquinone2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity. |
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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. |
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S5266 |
StiripentolStiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450. |
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S5252 |
Ozagrel sodiumOzagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties. |
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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. |
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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. |
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S5658 |
Omeprazole SodiumOmeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19. |
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S7456 |
Osilodrostat (LCI699)LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis. |
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S2380 |
DiosmetinDiosmetin (Luteolin 4-methyl ether) is a bioflavonoid found in spearmint, oregano, and many other plants. |
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S2262 |
ApigeninApigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM. |
![]() ![]() Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration. |
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S4938 |
CedrolCedrol, 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. |
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S2268 |
BaicaleinBaicalein is a CYP2C9 and prolyl endopeptidase inhibitor. |
![]() ![]() 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. |
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S2389 |
Naringin DihydrochalconeNaringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes. |
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S5416 |
MetyraponeMetyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis. |
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S2394 |
NaringeninNaringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol) 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. |
![]() ![]() (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.
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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. |
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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. |
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S3777 |
GentiopicrosideGentiopicroside (GE, Gentiopicrin), 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. |
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S2401 |
Sodium DanshensuSodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza. |
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S3931 |
Ginsenoside RdGinsenoside 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, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
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S4831 |
Piperonyl butoxidePiperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.Piperonyl butoxide is an inhibitor of cytochrome P450 monooxygenases(P450s). |
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S3673 |
SulfaphenazoleSulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) 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). |
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S3766 |
Tanshinone IIA sulfonate sodiumSodium 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) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). |
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S3917 |
TetrahydrocurcuminTetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4. |
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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. |
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S3660 |
UniconazoleUniconazole (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. |
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S2329 |
NaringinNaringin (Naringoside) 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. |
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S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein. |
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S4221 |
BenzbromaroneBenzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM. |
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S3719 |
TopiroxostatTopiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment. |
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S2344 |
PiperinePiperine (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. |
![]() ![]() 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.
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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. |
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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. |
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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. |
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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. |
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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). |
Catalog No. | Information | Product Use Citations | Product Validations |
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S2271 |
Berberine chlorideBerberine chloride (Natural Yellow 18 chloride) 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. |
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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 |
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S0110New |
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). |
Catalog No. | Information | Product Use Citations | Product Validations |
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S6606 |
CDD3505CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. |
Catalog No. | Information | Product Use Citations | Product Validations |
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S1442 |
VoriconazoleVoriconazole (UK-109496) 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. |
![]() ![]() 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. |
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S6790New |
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. |
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S1712 |
DeferasiroxDeferasirox (CGP-72670, ICL-670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death. |
![]() ![]() 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. |
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S4155 |
ChlorzoxazoneChlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1. |
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S4741 |
DanshensuDanshensu (Salvianic acid A), a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Danshensu inhibits CYP2E1 and CYP2C9 with IC50 of 36.63 and 75.76 μm, respectively. |