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 P450 (e.g. CYP17)抑制剂(40) P450 (e.g. CYP17)化学产品(3) 新P450 (e.g. CYP17)产品

产品目录	产品描述	文献引用	实验数据
S1123	Abiraterone Abiraterone是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。	Nature, 2018, 560(7718):372-376 J Biol Chem, 2015, 290(6):3248-68 Chem Res Toxicol, 2012, 25(8):1720-31	A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.
S1185	Ritonavir Ritonavir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。	Blood, 2012, 119(20):4686-97 J Immunol, 2014, 192(8):3496-506 Antiviral Res, 2015, 120:140-6	(A) KMS11 and (B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown). (C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to untreated cells (not shown).
S2246	Abiraterone Acetate Abiraterone Acetate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。	Br J Cancer, 2018, 10.1038/s41416-018-0158-y J Biol Chem, 2015, 290(6):3248-68 Endocrinology, 2014, 155(2):358-69	Concomitant Western blot analysis of ER and TFF1 assessed after 16 h treatment with E2 or abiraterone in the presence or absence of MG-132 (10 μM).
S1257	Posaconazole Posaconazole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。	Antimicrob Agents Chemother, 2015, 59(5):2654-65 Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Eur J Pharm Sci, 2016, 10.1016/j.ejps.2016.05.009	Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
S1442	Voriconazole Voriconazole是一种三唑类抗真菌药物，用于治疗严重的侵入性真菌感染。	Antimicrob Agents Chemother, 2015, 59(5):2654-65 Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother, 2015, 59(9):5548-54	Voriconazole increases the osteogenic activity of human osteoblasts in vitro. Osteoblasts were exposed to voriconazole (VCZ) or fluconazole (FCZ) at 15 or 200 μg/ml in osteoinductive medium (OS+) for up to 7 days. As a positive control, cells were also exposed to sodium fluoride (NaF) at 10 μM in nonosteoinductive medium (OS−). Osteoblastic differentiation was evaluated by measuring alkaline phosphatase (ALP) activity (A) and staining for calcium deposition with alazarin red S stain (B and C); calcium deposition was quantified by measuring the absorbance (A415) of extracted alazarin red S (B) and was assessed by the light microscopic appearance (white arrows) of stained osteoblast cultures (C). Values represent the means ± SD. *, P < 0.05, compared to osteoblasts grown under osteogenic conditions without treatment.
S9257^New	Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
S9163^New	Rhapontigenin Rhapontigenin, produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S5380^New	7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5266^New	Stiripentol Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S5529^New	Galangin Galangin, a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S5429^New	Diallyl sulfide Diallyl sulfide, a thioether found naturally in garlic, is a selective inhibitor and also a substrate of CYP2E1 with an IC50 of 17.3 μM. It has protective effects against alcohol- and acetaminophen-induced hepatotoxicity in many studies.
S2187	Avasimibe Avasimibe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，	Nature, 2016, 531(7596):651-5 Oncogene, 2016, 35(50):6378-6388 Nanomedicine, 2018, 14(8):2541-2550	a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11).
S1353	Ketoconazole Ketoconazole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。	Cancer Manag Res, 2018, 10:4421-4438 Clin Cancer Res, 2017, 23(20):6203-6214
S2476	Itraconazole Itraconazole是一种三唑类抗真菌药物，是CYP3A4的有效抑制剂，IC50为6.1 nM。	Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother, 2015, 59(9):5548-54 Med Mycol, 2016, 10.1093/mmy/myw131	MCF-7 and SKBR-3 cells were treated as indicated and morphology of autophagosomes was observed with TEM (C). Autophagosomes (Avi, immature autophagic vacuoles, bold arrow), autolysosomes (Avd, degraded/late autophagic vacuoles, sharp arrow).
S1331	Fluconazole Fluconazole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。	Antimicrob Agents Chemother, 2015, 59(4):2388-97 Int J Antimicrob Agents, 2017, 49(6):740-748 Int J Antimicrob Agents, 2017, 10.1016/j.ijantimicag.2017.01.029
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel)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。Phase 3。	Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2803	Galeterone Galeterone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。	Biochem Biophys Res Commun, 2016, 477(4):1005-10 Steroids, 2018, 138:82-90	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S2555	Clarithromycin Clarithromycin 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。
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。	Antimicrob Agents Chem, 2017, 10.1128/AAC.01776-16	Effects of rifampin alone or in combination with cobicistat on the mean DRV CLint.app. in primary human hepatocytes in vitro. Cryopreserved primary human hepatocytes were incubated with RIF (0.5 to 20 μM) (hatched bars) or with COBI (0.13 to 12.76 μM) and RIF (0.5 to 20 μM) (gray bars) for 72 h. All cells were then incubated with RIF (0.5 to 20 M) or RIF (0.5 to 20 μM) together with COBI (0.13 to 12.76 μM), as described above, together with DRV (5 μM) for 60 min. Control cells were treated with DRV (5 μM) alone for 60 min (black bar). The results shown represent the mean DRV CLint.app. from three biological replicates measured in hepatocytes from three independent donors (donors HU1399, HU1574, and HU1587). Error bars indicate SDs.
S2496	Ozagrel Ozagrel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是Pioglitazone的盐酸盐形式，是细胞色素P450 (CYP)2C8和CYP3A4酶抑制剂，作用于CYP2C8， CYP3A4和CYP2C9， K_i分别为1.7 μM， 11.8 μM和32.1 μM。	Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2067	Ozagrel HCl Ozagrel HCl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。
S2526	Alizarin Alizarin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。
S2921	PF-4981517 PF-4981517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。
S2043	Memantine HCl Memantine HCl是一种CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，K_i分别为0.51 nM和94.9 μM。
S2380	Diosmetin Diosmetin 是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。
S2262	Apigenin Apigenin是一种有效的CYP2C9抑制剂，K_i为2 μM.。	Oncol Rep, 2015, 34(4):1805-14 Int J Clin Exp Pathol, 2014, 7(7):3938-3947 Oxid Med Cell Longev, 2017, 2017:4397340	SKH-1 mice were subjected to UVB radiation (1000 J/m2 daily, 5 days), or topical apigenin (Api, 5 μmol, in 200 μl vehicle, DMSO: acetone 1:9) was applied 1 h prior to each UVB exposure. Mice were also sham-irradiated and treated with apigenin, and the control group of mice was subjected to sham irradiation and vehicle. 24 h after the final UVB exposure, the mice were euthanized, dorsal skin was harvested, fixed in formalin and paraffin-embedded. (A) Representative Hematoxylin and Eosin (H&E) staining of skin sections (scale bar, 100 μm). (B) Quantitation of epidermal thickness (mean ± SD), , P < 0.001; *, P< 0.0001. Three sections per mouse and 3 mice per group were evaluated.
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。	J Nutr Biochem, 2013, 24(11):1953-62 Mol Cell Biochem, 2015, 10.1007/s11010-015-2429-8 Biochem Biophys Res Commun, 2016, 473(4):775-80	NKILA stably overexpressed and control SMMC-7721 and HepG2 cells were treated with a series dose of Baicalein (0, 12.5, 25, 50, 100 μM) for 48 h. Then, cell proliferation was detected by Glo cell viability assays. The control condition was defined as media alone with no NKILA overexpression.
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。
S2394	Naringenin Naringenin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。	Sci Rep, 2016, 6:27268	(d) Antiviral activity of SZA on assembly and release. Huh7 cells were electroporated with JFH-1 RNA of HCV, followed by 4 h treatment of the indicated concentrations of SZA. At 48 h after electroporation, cells were subjected to three cycles of freeze and thaw to test the intracellular viral infectivity; supernatants of the electroporated cells were collected for the detection of extracellular viral infectivity. 100 μM naringenin was introduced as a positive control. Results are shown as relative HCV infectivity compared to DMSO treated group. Data shown as mean ± SD of three independent experiments.
S3777	Gentiopicroside Gentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S2401	Sodium Danshensu Sodium Danshensu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。
S3673	Sulfaphenazole Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
S3660	Uniconazole Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis.
S2329	Naringin Naringin 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。
S4221	Benzbromarone Benzbromarone 是CYP2C9抑制剂，与CYP2C9 结合，K_i为19.3 nM。
S2344	Piperine Piperine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.
S1712	Deferasirox Deferasirox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。	Nature, 2014, 509(7498):105-9	U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox.
S4155	Chlorzoxazone Chlorzoxazone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(丹参素)，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。

产品目录	产品描述	文献引用	实验数据
S1123	Abiraterone Abiraterone是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。	Nature,2018, 560(7718):372-376 J Biol Chem,2015, 290(6):3248-68 Chem Res Toxicol,2012, 25(8):1720-31	A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.
S1185	Ritonavir Ritonavir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。	Blood,2012, 119(20):4686-97 J Immunol,2014, 192(8):3496-506 Antiviral Res,2015, 120:140-6	(A) KMS11 and (B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown). (C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to untreated cells (not shown).
S2246	Abiraterone Acetate Abiraterone Acetate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。	Br J Cancer,2018, 10.1038/s41416-018-0158-y J Biol Chem,2015, 290(6):3248-68 Endocrinology,2014, 155(2):358-69	Concomitant Western blot analysis of ER and TFF1 assessed after 16 h treatment with E2 or abiraterone in the presence or absence of MG-132 (10 μM).
S1257	Posaconazole Posaconazole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。	Antimicrob Agents Chemother,2015, 59(5):2654-65 Antimicrobial Agents and Chemotherapy,2016, 10.1128/AAC.02921-15 Eur J Pharm Sci,2016, 10.1016/j.ejps.2016.05.009	Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
S1442	Voriconazole Voriconazole是一种三唑类抗真菌药物，用于治疗严重的侵入性真菌感染。	Antimicrob Agents Chemother,2015, 59(5):2654-65 Antimicrobial Agents and Chemotherapy,2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother,2015, 59(9):5548-54	Voriconazole increases the osteogenic activity of human osteoblasts in vitro. Osteoblasts were exposed to voriconazole (VCZ) or fluconazole (FCZ) at 15 or 200 μg/ml in osteoinductive medium (OS+) for up to 7 days. As a positive control, cells were also exposed to sodium fluoride (NaF) at 10 μM in nonosteoinductive medium (OS−). Osteoblastic differentiation was evaluated by measuring alkaline phosphatase (ALP) activity (A) and staining for calcium deposition with alazarin red S stain (B and C); calcium deposition was quantified by measuring the absorbance (A415) of extracted alazarin red S (B) and was assessed by the light microscopic appearance (white arrows) of stained osteoblast cultures (C). Values represent the means ± SD. *, P < 0.05, compared to osteoblasts grown under osteogenic conditions without treatment.
S9257^New	Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
S9163^New	Rhapontigenin Rhapontigenin, produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S5380^New	7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5266^New	Stiripentol Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S5529^New	Galangin Galangin, a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S5429^New	Diallyl sulfide Diallyl sulfide, a thioether found naturally in garlic, is a selective inhibitor and also a substrate of CYP2E1 with an IC50 of 17.3 μM. It has protective effects against alcohol- and acetaminophen-induced hepatotoxicity in many studies.
S2187	Avasimibe Avasimibe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，	Nature,2016, 531(7596):651-5 Oncogene,2016, 35(50):6378-6388 Nanomedicine,2018, 14(8):2541-2550	a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11).
S1353	Ketoconazole Ketoconazole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。	Cancer Manag Res,2018, 10:4421-4438 Clin Cancer Res,2017, 23(20):6203-6214
S2476	Itraconazole Itraconazole是一种三唑类抗真菌药物，是CYP3A4的有效抑制剂，IC50为6.1 nM。	Antimicrobial Agents and Chemotherapy,2016, 10.1128/AAC.02921-15 Antimicrob Agents Chemother,2015, 59(9):5548-54 Med Mycol,2016, 10.1093/mmy/myw131	MCF-7 and SKBR-3 cells were treated as indicated and morphology of autophagosomes was observed with TEM (C). Autophagosomes (Avi, immature autophagic vacuoles, bold arrow), autolysosomes (Avd, degraded/late autophagic vacuoles, sharp arrow).
S1331	Fluconazole Fluconazole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。	Antimicrob Agents Chemother,2015, 59(4):2388-97 Int J Antimicrob Agents,2017, 49(6):740-748 Int J Antimicrob Agents,2017, 10.1016/j.ijantimicag.2017.01.029
S1195	TAK-700 (Orteronel) TAK-700 (Orteronel)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。Phase 3。	Biochem Biophys Res Commun,2016, 477(4):1005-10
S2803	Galeterone Galeterone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。	Biochem Biophys Res Commun,2016, 477(4):1005-10 Steroids,2018, 138:82-90	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S2555	Clarithromycin Clarithromycin 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。
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。	Antimicrob Agents Chem,2017, 10.1128/AAC.01776-16	Effects of rifampin alone or in combination with cobicistat on the mean DRV CLint.app. in primary human hepatocytes in vitro. Cryopreserved primary human hepatocytes were incubated with RIF (0.5 to 20 μM) (hatched bars) or with COBI (0.13 to 12.76 μM) and RIF (0.5 to 20 μM) (gray bars) for 72 h. All cells were then incubated with RIF (0.5 to 20 M) or RIF (0.5 to 20 μM) together with COBI (0.13 to 12.76 μM), as described above, together with DRV (5 μM) for 60 min. Control cells were treated with DRV (5 μM) alone for 60 min (black bar). The results shown represent the mean DRV CLint.app. from three biological replicates measured in hepatocytes from three independent donors (donors HU1399, HU1574, and HU1587). Error bars indicate SDs.
S2496	Ozagrel Ozagrel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是Pioglitazone的盐酸盐形式，是细胞色素P450 (CYP)2C8和CYP3A4酶抑制剂，作用于CYP2C8， CYP3A4和CYP2C9， K_i分别为1.7 μM， 11.8 μM和32.1 μM。	Mol Nutr Food Res,2017, 10.1002/mnfr.201601075 Drug Metab Dispos,2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2067	Ozagrel HCl Ozagrel HCl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。
S2526	Alizarin Alizarin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。
S2921	PF-4981517 PF-4981517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。
S2043	Memantine HCl Memantine HCl是一种CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，K_i分别为0.51 nM和94.9 μM。
S2380	Diosmetin Diosmetin 是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。
S2262	Apigenin Apigenin是一种有效的CYP2C9抑制剂，K_i为2 μM.。	Oncol Rep,2015, 34(4):1805-14 Int J Clin Exp Pathol,2014, 7(7):3938-3947 Oxid Med Cell Longev,2017, 2017:4397340	SKH-1 mice were subjected to UVB radiation (1000 J/m2 daily, 5 days), or topical apigenin (Api, 5 μmol, in 200 μl vehicle, DMSO: acetone 1:9) was applied 1 h prior to each UVB exposure. Mice were also sham-irradiated and treated with apigenin, and the control group of mice was subjected to sham irradiation and vehicle. 24 h after the final UVB exposure, the mice were euthanized, dorsal skin was harvested, fixed in formalin and paraffin-embedded. (A) Representative Hematoxylin and Eosin (H&E) staining of skin sections (scale bar, 100 μm). (B) Quantitation of epidermal thickness (mean ± SD), , P < 0.001; *, P< 0.0001. Three sections per mouse and 3 mice per group were evaluated.
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。	J Nutr Biochem,2013, 24(11):1953-62 Mol Cell Biochem,2015, 10.1007/s11010-015-2429-8 Biochem Biophys Res Commun,2016, 473(4):775-80	NKILA stably overexpressed and control SMMC-7721 and HepG2 cells were treated with a series dose of Baicalein (0, 12.5, 25, 50, 100 μM) for 48 h. Then, cell proliferation was detected by Glo cell viability assays. The control condition was defined as media alone with no NKILA overexpression.
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。
S2394	Naringenin Naringenin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。	Sci Rep,2016, 6:27268	(d) Antiviral activity of SZA on assembly and release. Huh7 cells were electroporated with JFH-1 RNA of HCV, followed by 4 h treatment of the indicated concentrations of SZA. At 48 h after electroporation, cells were subjected to three cycles of freeze and thaw to test the intracellular viral infectivity; supernatants of the electroporated cells were collected for the detection of extracellular viral infectivity. 100 μM naringenin was introduced as a positive control. Results are shown as relative HCV infectivity compared to DMSO treated group. Data shown as mean ± SD of three independent experiments.
S3777	Gentiopicroside Gentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S2401	Sodium Danshensu Sodium Danshensu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。
S3673	Sulfaphenazole Sulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
S3660	Uniconazole Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis.
S2329	Naringin Naringin 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。
S4221	Benzbromarone Benzbromarone 是CYP2C9抑制剂，与CYP2C9 结合，K_i为19.3 nM。
S2344	Piperine Piperine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.

产品目录	产品描述	文献引用	实验数据
S1712	Deferasirox Deferasirox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。	Nature, 2014, 509(7498):105-9	U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox.
S4155	Chlorzoxazone Chlorzoxazone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(丹参素)，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。

产品目录

产品描述

文献引用

实验数据

S1712