P450 (e.g. CYP17)

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

P450 (e.g. CYP17)产品

所有产品(80) P450 (e.g. CYP17)抑制剂(69) P450 (e.g. CYP17)激活剂(4) P450 (e.g. CYP17)调节剂(2)

目录号	产品描述	文献引用	实验数据
S1123	Abiraterone (CB-7598) Abiraterone (CB-7598) 是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。	Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765 J Biol Chem, 2021, 297(2):100969	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
S1185	Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel)是Cytochrome P450 3A和HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein，诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。	mBio, 2021, 12(1)e02754-20 Cell Chem Biol, 2021, S2451-9456(21)00441-4 J Antimicrob Chemother, 2021, 76(7):1874-1885	(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 tountreated cells (not shown).
S2246	Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630)是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂，无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。	Clin Cancer Res, 2021, clincanres.4391.2020 Neoplasia, 2021, 23(12):1261-1274 J Biol Chem, 2021, 297(2):100969	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.
S1257	Posaconazole (SCH 56592) Posaconazole (SCH56592) 是CYP3A4的抑制剂，但不抑制其他CYP酶的活性；同时是sterol C14ɑ demethylase的抑制剂，IC50为0.25 μM。其平均的消除半衰期为15-35小时。	Front Microbiol, 2021, 12:649026 J Ind Microbiol Biotechnol, 2021, kuab079 Clin Exp Pharmacol Physiol, 2021, 10.1111/1440-1681.13475	Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) orextreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
S6437^New	Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate 是一种止咳药，是 CYP2B1/2 的抑制剂。Oxolamine citrate 也表现出抗炎作用。
S2187	Avasimibe (CI-1011) Avasimibe (CI-1011, PD-148515) 抑制ACAT，IC50为3.3 μM，也抑制人P450同工酶CYP2C9， CYP1A2和CYP2C19，IC50分别为2.9 μM， 13.9 μM和26.5 μM，	Nat Commun, 2021, 12(1):2814 Cell Chem Biol, 2021, S2451-9456(21)00213-0 Cell Death Discov, 2021, 7(1):38	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 (R 41400) Ketoconazole (R 41400)能抑制cyclosporine oxidase（环孢素氧化酶）和testosterone 6 beta-hydroxylase（睾丸素6β-羟化酶），IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Nat Commun, 2021, 12(1):652 Pharmacol Res, 2021, 169:105648
S2476	Itraconazole (R 51211) Itraconazole (R 51211) 是一种三唑类抗真菌药物，是CYP3A4的有效抑制剂，IC50为6.1 nM。Itraconazole 是一个有效的Hedgehog (Hh)信号通路的拮抗剂。Itraconazole 可通过诱导自噬来抑制恶性胶质瘤的生长。	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Sci Rep, 2021, 11(1):17665 Front Microbiol, 2021, 12:649026	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 (UK 49858) Fluconazole (UK 49858)是一种羊毛甾醇14 alpha去甲基化酶抑制剂，抑制了麦角固醇的形成，用于治疗和预防浅表性和全身性真菌感染。	Front Microbiol, 2021, 12:649026 ACS Omega, 2021, 6(12):8477-8487 PLoS Pathog, 2020, 16;16(3):e1008341
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel) 是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。	Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2803	Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534 Steroids, 2018, 129:24-34	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.
S4202	Verapamil (CP-16533-1) HCl Verapamil HCl (CP-16533-1)是L-型钙通道抑制剂，是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。	ACS Nano, 2021, 10.1021/acsnano.1c03517 Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y Eur J Med Chem, 2021, 218:113403	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.
S2555	Clarithromycin Clarithromycin (A-56268) 是一种大环内酯类抗生素，是CYP3A4抑制剂，用于治疗许多细菌感染。	Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5 J Ovarian Res, 2019, 12(1):107 J Med Chem, 2018, 61(9):4189-4202
S2900	Cobicistat (GS-9350) Cobicistat (GS-9350)是一种有效的CYP3A选择性抑制剂，IC50为30 - 285 nM。	Hum Cell, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4 Cancer Cell Int, 2020, 19;20:58	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 (OKY-046)是一种有效的，选择性的血栓素A2合成酶抑制剂，IC50为4 nM。
S1739	Thiabendazole Thiabendazole 抑制线粒体蠕虫特异性酶，延胡索酸还原酶，具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。
S2046	Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂，对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。	J Nanobiotechnology, 2021, 19(1):150 Biol Pharm Bull, 2019, 42(8):1303-1309 Nan Fang Yi Ke Da Xue Xue Bao, 2019, 39(1):23-29	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 (OKY-046)是选择性血栓素A2合成酶抑制剂，其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩，以及伴随的脑梗塞。
S1952	Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) 是在一些植物中发现的天然存在的呋喃香豆素化合物，包括补骨脂，用于治疗牛皮癣，湿疹，白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。	Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58
S2526	Alizarin Alizarin (Anthraquinonic) 强效抑制P450亚型CYP1A1， CYP1A2和CYP1B1，IC50分别为6.2 μM， 10.0 μM and 2.7 μM，微弱抑制CYP2A6和CYP2E1，对CYP2C19，对CYP3A4和CYP3A5没有抑制作用。	Cell Rep, 2020, 14;31(2):107518 Biomaterials, 2019, 192:323-333
S1794	Fenofibrate (NSC-281319) Fenofibrate (NSC-281319)是一种Fibrate类化合物，是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂，EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ，对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。	Redox Biol, 2021, 46:102082 J Cell Mol Med, 2020, 24(6):3384-3398 J Cell Mol Med, 2020, 24(6):3384-3398	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.
S5169	2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721	Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂，Ki值为0.2 μM。
S2921	PF-4981517 PF-4981517 (CYP3cide, PF-04981517) 是一种有效的，选择性的CYP3A4(P450)抑制剂，IC50为0.03 μM，比作用于CYP3A5和CYP3A7选择性高500倍以上。
S5266	Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S3273	Hypericin Hypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质，具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)、PKC (protein kinase C)、dopamine-beta-hydroxylase、reverse transcriptase、telomerase 和 CYP (cytochrome P450)。	Eur J Pharmacol, 2021, 900:174071
S3291	Myristicin Myristicin (Myristicine) 是一种在 Myristica fragrans 的种子 Nutmeg 中的萜烯样活性成分，是 monamine oxidase (MAO) 的弱抑制剂和 CYP1A2 的机理抑制剂。
S5252	Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
S0541	Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效，选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生，其IC50值为0.3 μM，并可平行地增强 PGE2 的产生。
S9250	Isosilybin Isosilybin (Silymarin, Silybin B, Isosilybinin, Q-100795)是一种在水飞蓟(S. marianum)果实提取物中发现的黄烷醇，具有抗氧化和抗癌活性。Isosilybin 抑制 CYP3A4 诱导，IC50为74 μM。
S9257	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.
S5658	Omeprazole Sodium Omeprazole 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.	Theranostics, 2021, 11(5):2364-2380 J Virol, 2021, JVI.00190-21 Biosci Rep, 2021, BSR20200842
S7456	Osilodrostat (LCI699) LCI699 (Osilodrostat) 是有效的11β-hydroxylase (CYP11B)抑制剂，11β-hydroxylase是催化皮质醇合成的最后一步。	J Biol Chem, 2021, S0021-9258(21)00587-1
S2380	Diosmetin Diosmetin (Luteolin 4-methyl ether)是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。	Mol Med Rep, 2020, 22(2):1335-1341 Br J Pharmacol, 2019, 176(12):2079-2094 Int J Biol Sci, 2019, 15(11):2497-2508
S2262	Apigenin (LY 080400) Apigenin (NSC 83244, LY 080400)是一种有效的CYP2C9抑制剂，K_i为2 μM.。	Cancer Lett, 2021, 515:36-48 Front Cell Infect Microbiol, 2021, 11:630812 Molecules, 2021, 26(5)1210	Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration.
S4938	Cedrol Cedrol是一种天然存在的倍半萜烯醇，是有效的、竞争性的抑制剂，抑制CYP2B6介导的安非他酮羟化酶(bupropion hydroxylase)，Ki值为0.9 μM。它还能抑制CYP3A4介导的咪达唑仑羟基化，Ki为3.4 μM。对CYP2C8, CYP2C9和CYP2C19的活性仅有微弱的抑制作用。
S2268	Baicalein Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。	Free Radic Biol Med, 2021, 163:234-242 Molecules, 2021, 26(5)1210 Autophagy, 2020, 16;1-15	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 是一种新型甜味剂，是来自柚皮苷的一种人工甜味剂。也是一种CYP enzymes的抑制剂。
S5416	Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
S2394	Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol)是来自于食用植物的一种天然的主要黄酮类化合物，有益人体健康，具有生物活性，是一种抗氧化剂，自由基清除剂，抗炎，碳水化合物代谢启动子及免疫系统的调制剂。	Eur J Pharmacol, 2020, 173323 Int J Mol Sci, 2020, 21(14):5025 Biomed Pharmacother, 2019, 115:108848	(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.
S9299	Ginsenoside F1 Ginsenoside F1 是人参的药物成分，已知具有抗衰老、抗氧化、抗癌和角质形成细胞的保护作用。Ginsenoside F1 对 CYP3A4 活性具有竞争性抑制作用，Ki值为67.8 ± 16.2 μM。Ginsenoside F1 对 CYP2D6 的抑制作用较弱。
S4963	Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin)是从茜草根和其他茜草科植物家族中分离出的天然色素。它具有抗血管生成、抗菌、抗氧化活性。Purpurin 可有效地抑制CYP1A1、CYP1A2 和 CYP1B1。
S3777	Gentiopicroside Gentiopicroside (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.
S0110	APD597 APD-597 (JNJ-38431055) 是一种有效的、选择性的 G protein-coupled receptor 119 (GPR119) 的激动剂，对hGPR119的EC50值为46 nM，也是 Cytochrome P450 2C9 (CYP2C9) 的抑制剂，IC50值为5.8 μM。APD-597 (JNJ-38431055) 被开发用于治疗2型糖尿病(T2D)。
S2401	Sodium Danshensu Sodium Danshensu是丹参素的单钠盐，是从Salvia miltiorrhiza Bge中分离的天然酚酸，是咖啡酸衍生物。	J Med Virol, 2019, 91(8):1440-1447
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, 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.	J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S4831	Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606)是一种人造的农药增效剂，与杀虫剂一起作用能够增强其有效性。
S3673	Sulfaphenazole Sulfaphenazole (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).
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) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
S3917	Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.
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.	J Bone Miner Res, 2021, 10.1002/jbmr.4328 Int J Mol Med, 2021, 48(4)192
S3660	Uniconazole (S 3307D) Uniconazole (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.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S2329	Naringin Naringin (Naringoside) 是一种黄酮苷，是葡萄柚中的主要的类黄酮，具有柚子汁的苦味。具有抗氧化，降血脂，抗肿瘤活性，并且对cytochrome P450有抑制作用。	Am J Transl Res, 2021, 13(6):6330-6341 Int J Mol Sci, 2020, 21(14):5025
S4662	Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂，也是 P-glycoprotein 的抑制剂和诱导剂。	Sci Rep, 2021, 11(1):19443 Front Cardiovasc Med, 2021, 8:634774 ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536
S0175	DMU2105 DMU2105 是一种有效且特异的 CYP1B1 抑制剂，其IC50值为10 nM。
S0176	DMU2139 DMU2139 是一种有效且特异的 CYP1B1 抑制剂，其IC50值为9 nM。
S4221	Benzbromarone Benzbromarone 是CYP2C9抑制剂，与CYP2C9 结合，K_i为19.3 nM。	Hum Mol Genet, 2020, ddaa244
S3719	Topiroxostat Topiroxostat 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.
S2344	Piperine Piperine (1-Piperoylpiperidine) 是一种生物碱，是造成黑胡椒和长胡椒辛辣的原因，也用于一些传统医学领域，且作为杀虫剂。	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.
S6886	1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) 是一种非选择性且不可逆的 cytochrome P450 (CYP) enzymes 的抑制剂。1-Aminobenzotriazole 还是 N-acetyltransferase (NAT) 的底物和抑制剂。
S9442	Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin)是在柠檬、佛手柑等柑橘精油中发现的天然呋喃香豆素。Bergaptol 是有效的 CYP3A4 酶脱苄基活性抑制剂，IC50值为24.92 μM。
S5380	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.
S5529	Galangin Galangin (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.
S2274	TMS TMS是一种有效的、选择性的、竞争性的 cytochrome P450 1B1 (CYP1B1) 抑制剂，IC50为6 nM。TMS对P450 1B1的选择性是P450 1A1（IC50为300 nM）的50倍，对P450 1A2（IC50为3μM）的选择性是500倍。
S5429	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.
S9241	Polygalaxanthone III Polygalaxanthone III 是一种天然产物，具有镇静，减轻感冒，消除痰液和消肿的功效。Polygalaxanthone III 抑制 CYP2E1 催化的氯唑沙宗6-羟基化反应，IC50值为50.56 μM。
S9163	Rhapontigenin Rhapontigenin (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).
S0230	NVP-VID-400 NVP-VID-400 (SDZ285428) 是 CYP51 的抑制剂。NVP-VID-400 (SDZ285428) 抑制 T. cruzi 和 T. brucei 的I/E₂^a(5 min) 值均 <1 而 I/E₂(60 min) 值分别为9和35。
S3227	5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) 是一种 cytochrome P450 (CYP) 3As 的抑制剂，可显著地降低肝脏中CYP3A11和CYP3A25的表达。5,7-Dimethoxyflavone (5,7-DMF) 也是一种有效的 Breast Cancer Resistance Protein (BCRP, ABCG2) 的抑制剂。5,7-Dimethoxyflavone (5,7-DMF) 是Kaempferia parviflora的主要成分之一，具有抗肥胖、抗炎和抗肿瘤作用。
S5967^New	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8，poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。	Front Pharmacol, 2021, 12:632201
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8，分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1，Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
S6868	Alflutinib (AST2818) mesylate Alflutinib (AST2818, Furmonertinib) mesylate 是第三代 epidermal growth factor receptor (EGFR) 的抑制剂，可抑制EGFR敏感突变和T790M突变。Alflutinib (AST2818) 主要由CYP3A4代谢，也是有效的 CYP3A4 的诱导剂，EC50值为0.25 μM。
S4784	Phloracetophenone Phloracetophenone, 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).
S5969^New	Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil) 是一种青霉素类的窄谱β-内酰胺抗生素，可在临床上水平上诱导药物代谢有关的 CYP enzymes 水平。
S6606	CDD3505 CDD3505可通过诱导肝脏细胞色素P450IIIA活性，提高高密度脂蛋白胆固醇（HDL）水平。
S1442	Voriconazole (UK-109496) Voriconazole (UK-109496) 是类似于氟康唑和伊曲康唑的新型三唑衍生物，其作用是通过抑制真菌 cytochrome P-450 依赖性的，14-alpha-sterol demethylase 介导的麦角固醇的合成。	Front Microbiol, 2021, 12:649026 Antimicrob Agents Chemother, 2020, 6 pii: AAC Front Microbiol, 2020, 11:579362	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.
S1712	Deferasirox (ICL-670) Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂，是cytochrome P450 3A4诱导剂，Cytochrome P450 2C8的抑制剂，Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。	Br J Haematol, 2021, 192(4):747-760 J Transl Med, 2021, 19(1):347 Int J Mol Sci, 2020, 21(20)E7674	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是一种肌肉松弛的药物，作为人体肝脏细胞色素P-450IIE1的探针。
S4741	Danshensu Danshensu (Salvianic acid A)，是一种传统中药中的中草药，具有潜在的抗肿瘤和抗血管生成的效果。Danshensu 可抑制 CYP2E1 和 CYP2C9，对应的IC50值分别为36.63 μm和 75.76 μm。
S6790	Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE)是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

目录号	产品描述	文献引用	实验数据
S1123	Abiraterone (CB-7598) Abiraterone (CB-7598) 是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。Abiraterone (CB-7598) 是一种雄性激素 androgen 生物合成抑制剂。	Cancers (Basel),2021, 13(16)3959 Sci Rep,2021, 11(1):10765 J Biol Chem,2021, 297(2):100969	Inhibition study of expressed orendogenous 5α-reductase-3 enzymeintheabsenceandpresence of 100 and150 nM abiraterone at pH7.4 using 1.0 μM testosterone as substrate.
S1185	Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel)是Cytochrome P450 3A和HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein，诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。	mBio,2021, 12(1)e02754-20 Cell Chem Biol,2021, S2451-9456(21)00441-4 J Antimicrob Chemother,2021, 76(7):1874-1885	(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 tountreated cells (not shown).
S2246	Abiraterone Acetate (CB7630) Abiraterone Acetate (CB7630)是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂，无细胞试验中IC50为72 nM。Abiraterone acetateis 是一种口服的雄性激素 androgen 生物合成抑制剂。	Clin Cancer Res,2021, clincanres.4391.2020 Neoplasia,2021, 23(12):1261-1274 J Biol Chem,2021, 297(2):100969	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.
S1257	Posaconazole (SCH 56592) Posaconazole (SCH56592) 是CYP3A4的抑制剂，但不抑制其他CYP酶的活性；同时是sterol C14ɑ demethylase的抑制剂，IC50为0.25 μM。其平均的消除半衰期为15-35小时。	Front Microbiol,2021, 12:649026 J Ind Microbiol Biotechnol,2021, kuab079 Clin Exp Pharmacol Physiol,2021, 10.1111/1440-1681.13475	Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) orextreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
S6437^New	Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate 是一种止咳药，是 CYP2B1/2 的抑制剂。Oxolamine citrate 也表现出抗炎作用。
S2187	Avasimibe (CI-1011) Avasimibe (CI-1011, PD-148515) 抑制ACAT，IC50为3.3 μM，也抑制人P450同工酶CYP2C9， CYP1A2和CYP2C19，IC50分别为2.9 μM， 13.9 μM和26.5 μM，	Nat Commun,2021, 12(1):2814 Cell Chem Biol,2021, S2451-9456(21)00213-0 Cell Death Discov,2021, 7(1):38	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 (R 41400) Ketoconazole (R 41400)能抑制cyclosporine oxidase（环孢素氧化酶）和testosterone 6 beta-hydroxylase（睾丸素6β-羟化酶），IC50分别为0.19 mM和0.22 mM。Ketoconazole 是一种雄性激素 androgen 生物合成抑制剂。	Nat Biotechnol,2021, 10.1038/s41587-021-00860-4 Nat Commun,2021, 12(1):652 Pharmacol Res,2021, 169:105648
S2476	Itraconazole (R 51211) Itraconazole (R 51211) 是一种三唑类抗真菌药物，是CYP3A4的有效抑制剂，IC50为6.1 nM。Itraconazole 是一个有效的Hedgehog (Hh)信号通路的拮抗剂。Itraconazole 可通过诱导自噬来抑制恶性胶质瘤的生长。	Nat Biotechnol,2021, 10.1038/s41587-021-00860-4 Sci Rep,2021, 11(1):17665 Front Microbiol,2021, 12:649026	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 (UK 49858) Fluconazole (UK 49858)是一种羊毛甾醇14 alpha去甲基化酶抑制剂，抑制了麦角固醇的形成，用于治疗和预防浅表性和全身性真菌感染。	Front Microbiol,2021, 12:649026 ACS Omega,2021, 6(12):8477-8487 PLoS Pathog,2020, 16;16(3):e1008341
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel) 是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。Phase 3。	Drug Metab Dispos,2017, 45(6):635-645 Biochem Biophys Res Commun,2016, 477(4):1005-10
S2803	Galeterone Galeterone (TOK-001)是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	Cancer Chemother Pharmacol,2020, 10.1007/s00280-020-04195-w Steroids,2020, 153:108534 Steroids,2018, 129:24-34	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.
S4202	Verapamil (CP-16533-1) HCl Verapamil HCl (CP-16533-1)是L-型钙通道抑制剂，是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。	ACS Nano,2021, 10.1021/acsnano.1c03517 Cell Biol Toxicol,2021, 10.1007/s10565-021-09615-y Eur J Med Chem,2021, 218:113403	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.
S2555	Clarithromycin Clarithromycin (A-56268) 是一种大环内酯类抗生素，是CYP3A4抑制剂，用于治疗许多细菌感染。	Cell Biol Toxicol,2021, 10.1007/s10565-021-09646-5 J Ovarian Res,2019, 12(1):107 J Med Chem,2018, 61(9):4189-4202
S2900	Cobicistat (GS-9350) Cobicistat (GS-9350)是一种有效的CYP3A选择性抑制剂，IC50为30 - 285 nM。	Hum Cell,2021, 10.1007/s13577-021-00579-z Hum Cell,2021, 10.1007/s13577-021-00639-4 Cancer Cell Int,2020, 19;20:58	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 (OKY-046)是一种有效的，选择性的血栓素A2合成酶抑制剂，IC50为4 nM。
S1739	Thiabendazole Thiabendazole 抑制线粒体蠕虫特异性酶，延胡索酸还原酶，具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。
S2046	Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂，对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。	J Nanobiotechnology,2021, 19(1):150 Biol Pharm Bull,2019, 42(8):1303-1309 Nan Fang Yi Ke Da Xue Xue Bao,2019, 39(1):23-29	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 (OKY-046)是选择性血栓素A2合成酶抑制剂，其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩，以及伴随的脑梗塞。
S1952	Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) 是在一些植物中发现的天然存在的呋喃香豆素化合物，包括补骨脂，用于治疗牛皮癣，湿疹，白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。	Hum Cell,2021, 10.1007/s13577-021-00639-4 Hum Cell,2021, 10.1007/s13577-021-00579-z Cancer Cell Int,2020, 19;20:58
S2526	Alizarin Alizarin (Anthraquinonic) 强效抑制P450亚型CYP1A1， CYP1A2和CYP1B1，IC50分别为6.2 μM， 10.0 μM and 2.7 μM，微弱抑制CYP2A6和CYP2E1，对CYP2C19，对CYP3A4和CYP3A5没有抑制作用。	Cell Rep,2020, 14;31(2):107518 Biomaterials,2019, 192:323-333
S1794	Fenofibrate (NSC-281319) Fenofibrate (NSC-281319)是一种Fibrate类化合物，是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂，EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ，对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。	Redox Biol,2021, 46:102082 J Cell Mol Med,2020, 24(6):3384-3398 J Cell Mol Med,2020, 24(6):3384-3398	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.
S5169	2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721	Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) 是一种 adenosine diphosphate (ADP) 诱导的 platelet aggregation 的口服活性抑制剂。Ticlopidine 也是 CYP2B6 的抑制剂，Ki值为0.2 μM。
S2921	PF-4981517 PF-4981517 (CYP3cide, PF-04981517) 是一种有效的，选择性的CYP3A4(P450)抑制剂，IC50为0.03 μM，比作用于CYP3A5和CYP3A7选择性高500倍以上。
S5266	Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S3273	Hypericin Hypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质，具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)、PKC (protein kinase C)、dopamine-beta-hydroxylase、reverse transcriptase、telomerase 和 CYP (cytochrome P450)。	Eur J Pharmacol,2021, 900:174071
S3291	Myristicin Myristicin (Myristicine) 是一种在 Myristica fragrans 的种子 Nutmeg 中的萜烯样活性成分，是 monamine oxidase (MAO) 的弱抑制剂和 CYP1A2 的机理抑制剂。
S5252	Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
S0541	Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效，选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生，其IC50值为0.3 μM，并可平行地增强 PGE2 的产生。
S9250	Isosilybin Isosilybin (Silymarin, Silybin B, Isosilybinin, Q-100795)是一种在水飞蓟(S. marianum)果实提取物中发现的黄烷醇，具有抗氧化和抗癌活性。Isosilybin 抑制 CYP3A4 诱导，IC50为74 μM。
S9257	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.
S5658	Omeprazole Sodium Omeprazole 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.	Theranostics,2021, 11(5):2364-2380 J Virol,2021, JVI.00190-21 Biosci Rep,2021, BSR20200842
S7456	Osilodrostat (LCI699) LCI699 (Osilodrostat) 是有效的11β-hydroxylase (CYP11B)抑制剂，11β-hydroxylase是催化皮质醇合成的最后一步。	J Biol Chem,2021, S0021-9258(21)00587-1
S2380	Diosmetin Diosmetin (Luteolin 4-methyl ether)是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。	Mol Med Rep,2020, 22(2):1335-1341 Br J Pharmacol,2019, 176(12):2079-2094 Int J Biol Sci,2019, 15(11):2497-2508
S2262	Apigenin (LY 080400) Apigenin (NSC 83244, LY 080400)是一种有效的CYP2C9抑制剂，K_i为2 μM.。	Cancer Lett,2021, 515:36-48 Front Cell Infect Microbiol,2021, 11:630812 Molecules,2021, 26(5)1210	Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration.
S4938	Cedrol Cedrol是一种天然存在的倍半萜烯醇，是有效的、竞争性的抑制剂，抑制CYP2B6介导的安非他酮羟化酶(bupropion hydroxylase)，Ki值为0.9 μM。它还能抑制CYP3A4介导的咪达唑仑羟基化，Ki为3.4 μM。对CYP2C8, CYP2C9和CYP2C19的活性仅有微弱的抑制作用。
S2268	Baicalein Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。	Free Radic Biol Med,2021, 163:234-242 Molecules,2021, 26(5)1210 Autophagy,2020, 16;1-15	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 是一种新型甜味剂，是来自柚皮苷的一种人工甜味剂。也是一种CYP enzymes的抑制剂。
S5416	Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
S2394	Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol)是来自于食用植物的一种天然的主要黄酮类化合物，有益人体健康，具有生物活性，是一种抗氧化剂，自由基清除剂，抗炎，碳水化合物代谢启动子及免疫系统的调制剂。	Eur J Pharmacol,2020, 173323 Int J Mol Sci,2020, 21(14):5025 Biomed Pharmacother,2019, 115:108848	(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.
S9299	Ginsenoside F1 Ginsenoside F1 是人参的药物成分，已知具有抗衰老、抗氧化、抗癌和角质形成细胞的保护作用。Ginsenoside F1 对 CYP3A4 活性具有竞争性抑制作用，Ki值为67.8 ± 16.2 μM。Ginsenoside F1 对 CYP2D6 的抑制作用较弱。
S4963	Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin)是从茜草根和其他茜草科植物家族中分离出的天然色素。它具有抗血管生成、抗菌、抗氧化活性。Purpurin 可有效地抑制CYP1A1、CYP1A2 和 CYP1B1。
S3777	Gentiopicroside Gentiopicroside (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.
S0110	APD597 APD-597 (JNJ-38431055) 是一种有效的、选择性的 G protein-coupled receptor 119 (GPR119) 的激动剂，对hGPR119的EC50值为46 nM，也是 Cytochrome P450 2C9 (CYP2C9) 的抑制剂，IC50值为5.8 μM。APD-597 (JNJ-38431055) 被开发用于治疗2型糖尿病(T2D)。
S2401	Sodium Danshensu Sodium Danshensu是丹参素的单钠盐，是从Salvia miltiorrhiza Bge中分离的天然酚酸，是咖啡酸衍生物。	J Med Virol,2019, 91(8):1440-1447
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, 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.	J Ethnopharmacol,2021, S0378-8741(21)00169-0
S4831	Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606)是一种人造的农药增效剂，与杀虫剂一起作用能够增强其有效性。
S3673	Sulfaphenazole Sulfaphenazole (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).
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) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
S3917	Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties.
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.	J Bone Miner Res,2021, 10.1002/jbmr.4328 Int J Mol Med,2021, 48(4)192
S3660	Uniconazole (S 3307D) Uniconazole (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.	Nat Biotechnol,2021, 10.1038/s41587-021-00860-4
S2329	Naringin Naringin (Naringoside) 是一种黄酮苷，是葡萄柚中的主要的类黄酮，具有柚子汁的苦味。具有抗氧化，降血脂，抗肿瘤活性，并且对cytochrome P450有抑制作用。	Am J Transl Res,2021, 13(6):6330-6341 Int J Mol Sci,2020, 21(14):5025
S4662	Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂，也是 P-glycoprotein 的抑制剂和诱导剂。	Sci Rep,2021, 11(1):19443 Front Cardiovasc Med,2021, 8:634774 ACS Infect Dis,2020, 10.1021/acsinfecdis.0c00536
S0175	DMU2105 DMU2105 是一种有效且特异的 CYP1B1 抑制剂，其IC50值为10 nM。
S0176	DMU2139 DMU2139 是一种有效且特异的 CYP1B1 抑制剂，其IC50值为9 nM。
S4221	Benzbromarone Benzbromarone 是CYP2C9抑制剂，与CYP2C9 结合，K_i为19.3 nM。	Hum Mol Genet,2020, ddaa244
S3719	Topiroxostat Topiroxostat 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.
S2344	Piperine Piperine (1-Piperoylpiperidine) 是一种生物碱，是造成黑胡椒和长胡椒辛辣的原因，也用于一些传统医学领域，且作为杀虫剂。	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.
S6886	1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) 是一种非选择性且不可逆的 cytochrome P450 (CYP) enzymes 的抑制剂。1-Aminobenzotriazole 还是 N-acetyltransferase (NAT) 的底物和抑制剂。
S9442	Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin)是在柠檬、佛手柑等柑橘精油中发现的天然呋喃香豆素。Bergaptol 是有效的 CYP3A4 酶脱苄基活性抑制剂，IC50值为24.92 μM。
S5380	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.
S5529	Galangin Galangin (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.
S2274	TMS TMS是一种有效的、选择性的、竞争性的 cytochrome P450 1B1 (CYP1B1) 抑制剂，IC50为6 nM。TMS对P450 1B1的选择性是P450 1A1（IC50为300 nM）的50倍，对P450 1A2（IC50为3μM）的选择性是500倍。
S5429	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.
S9241	Polygalaxanthone III Polygalaxanthone III 是一种天然产物，具有镇静，减轻感冒，消除痰液和消肿的功效。Polygalaxanthone III 抑制 CYP2E1 催化的氯唑沙宗6-羟基化反应，IC50值为50.56 μM。
S9163	Rhapontigenin Rhapontigenin (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).
S0230	NVP-VID-400 NVP-VID-400 (SDZ285428) 是 CYP51 的抑制剂。NVP-VID-400 (SDZ285428) 抑制 T. cruzi 和 T. brucei 的I/E₂^a(5 min) 值均 <1 而 I/E₂(60 min) 值分别为9和35。
S3227	5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) 是一种 cytochrome P450 (CYP) 3As 的抑制剂，可显著地降低肝脏中CYP3A11和CYP3A25的表达。5,7-Dimethoxyflavone (5,7-DMF) 也是一种有效的 Breast Cancer Resistance Protein (BCRP, ABCG2) 的抑制剂。5,7-Dimethoxyflavone (5,7-DMF) 是Kaempferia parviflora的主要成分之一，具有抗肥胖、抗炎和抗肿瘤作用。

目录号	产品描述	文献引用
S5967^New	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8，poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。	Front Pharmacol, 2021, 12:632201
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8，分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1，Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
S6868	Alflutinib (AST2818) mesylate Alflutinib (AST2818, Furmonertinib) mesylate 是第三代 epidermal growth factor receptor (EGFR) 的抑制剂，可抑制EGFR敏感突变和T790M突变。Alflutinib (AST2818) 主要由CYP3A4代谢，也是有效的 CYP3A4 的诱导剂，EC50值为0.25 μM。
S4784	Phloracetophenone Phloracetophenone, 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).

目录号	产品描述	文献引用	实验数据
S5969^New	Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil) 是一种青霉素类的窄谱β-内酰胺抗生素，可在临床上水平上诱导药物代谢有关的 CYP enzymes 水平。
S6606	CDD3505 CDD3505可通过诱导肝脏细胞色素P450IIIA活性，提高高密度脂蛋白胆固醇（HDL）水平。

目录号

产品描述

文献引用

实验数据

S5969^New

Dicloxacillin Sodium hydrate

Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil) 是一种青霉素类的窄谱β-内酰胺抗生素，可在临床上水平上诱导药物代谢有关的 CYP enzymes 水平。

S6606

CDD3505

CDD3505可通过诱导肝脏细胞色素P450IIIA活性，提高高密度脂蛋白胆固醇（HDL）水平。

目录号	产品描述	文献引用	实验数据
S1442	Voriconazole (UK-109496) Voriconazole (UK-109496) 是类似于氟康唑和伊曲康唑的新型三唑衍生物，其作用是通过抑制真菌 cytochrome P-450 依赖性的，14-alpha-sterol demethylase 介导的麦角固醇的合成。	Front Microbiol, 2021, 12:649026 Antimicrob Agents Chemother, 2020, 6 pii: AAC Front Microbiol, 2020, 11:579362	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.
S1712	Deferasirox (ICL-670) Deferasirox (ICL-670, CGP-72670)是一种铁螯合剂，是cytochrome P450 3A4诱导剂，Cytochrome P450 2C8的抑制剂，Cytochrome P450 1A2抑制剂。Deferasirox 引起的铁损耗可促进BclxL下调和细胞死亡。	Br J Haematol, 2021, 192(4):747-760 J Transl Med, 2021, 19(1):347 Int J Mol Sci, 2020, 21(20)E7674	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是一种肌肉松弛的药物，作为人体肝脏细胞色素P-450IIE1的探针。
S4741	Danshensu Danshensu (Salvianic acid A)，是一种传统中药中的中草药，具有潜在的抗肿瘤和抗血管生成的效果。Danshensu 可抑制 CYP2E1 和 CYP2C9，对应的IC50值分别为36.63 μm和 75.76 μm。
S6790	Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE)是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

研究领域

产品类型

定制您的化合物库

P450 (e.g. CYP17)

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

P450 (e.g. CYP17)产品