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搜索结果：“AZ 960”

“AZ 960”的搜索结果

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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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AZD1480

Catalog No. A10110
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JAK 抑制剂

AZD1480是一种新型有效的小型JAK2抑制剂，IC50为0.26 nM。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。了解更多

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AZD8931 (Sapitinib)

Catalog No. A10116
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pan-EGFR/pan-erbB 抑制剂

AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。了解更多

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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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Thiazovivin

Catalog No. A10928
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ROCK 抑制剂

Thiazovivin是一种Rho相关激酶（ROCK）的选择性抑制剂。了解更多

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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

Product Citations (28)

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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AZD7762

Catalog No. A10113
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Chk1 & Chk2 抑制剂

AZD7762是一种有效的ATP竞争性检查点激酶抑制剂，可促进检查点废止并增强DNA靶向疗法。了解更多

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MK-1775

Catalog No. A10599
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WEE1 抑制剂

MK-1775是一种有效的体外和体内Wee1激酶抑制剂。了解更多

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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Dienogest

Catalog No. A10308
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Dienogest是一种口服抗孕激素，具有抗雄激素活性，因此可以改善雄激素症状。了解更多

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Voriconazole (Vfend)

Catalog No. A10978
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CYP17 抑制剂

Voriconazole (Vfend)是一种三唑抗真菌剂，可以冻干粉的形式用于静脉输注溶液。了解更多

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MLN2238 (Ixazomib)

Catalog No. A10600
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Proteasome 抑制剂

MLN2238 (Ixazomib)是20S蛋白酶体抑制剂的有效可逆特异性β5位点，IC50值为3.4 nM。了解更多

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Rosiglitazone maleate

Catalog No. A10809
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PPAR 激动剂

Rosiglitazone maleate是一种噻唑烷二酮类抗高血糖药，是PPARγ的高亲和、选择性的激动剂。了解更多

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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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Pyroxamide (NSC 696085)

Catalog No. A10764
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HDAC 抑制剂

Pyroxamide (NSC 696085)是亲和纯化的HDAC1的有效抑制剂，可导致乙酰化核心组蛋白在用该试剂培养的MEL细胞中积累。了解更多

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Fesoterodine fumarate (Toviaz)

Catalog No. A10386
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AChR 拮抗剂

Fesoterodine fumarate是一种用于尿急的药物，可减少尿液通过的频率并促使尿失禁。了解更多

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AZ 3146

Catalog No. A11170
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Mps1 抑制剂

AZ 3146是一种有效的选择性单极纺锤体1 (Mps1) 激酶抑制剂 (IC50 = 35 nM) 。它会干扰染色体对齐并覆盖纺锤体装配检查点，还抑制将Mad1，Mad2和着丝粒蛋白E（CENP-E）募集到动植物。了解更多

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- Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Kakihana A, .et al. Heat shock-induced mitotic arrest requires heat shock protein 105 for the activation of spindle assembly checkpoint, FASEB J, 2018, Nov 29:fj201801369R PMID: 30496702
- Suzuki M, .et al. Effect of MPS1 Inhibition on Genotoxic Stress Responses in Murine Tumour Cells, Anticancer Res, 2016, Jun;36(6):2783-92 PMID: 27272789
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YO-01027

Catalog No. A11174
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γ-secretase 抑制剂

YO-01027是一种二肽γ-secretase抑制剂，作用于APPL和Notch分裂，无细胞试验中IC50分别为2.6 nM和2.9 nM，一种抗阿尔茨海默氏病药物。了解更多

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Pazopanib HCl (GW786034)

Catalog No. A10699
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VEGFR/PDGFR/FGFR 抑制剂

Pazopanib HCl (GW786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Hideharu Yamada, .et al. lncRNA HAR1B has potential to be a predictive marker for pazopanib therapy in patients with sarcoma, Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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Posaconazole

Catalog No. A10744
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CYP3A4 抑制剂

Posaconazole主要是CYP3A4的抑制剂，但不抑制其他CYP酶的活性。也是甾醇C14+脱甲基酶抑制剂的抑制剂，IC50为0.25μM。泊沙康唑的终末消除半衰期中位数为15-35小时。了解更多

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Clozapine

Catalog No. A10236
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Clozapine是一种有效的5-HT1C受体拮抗剂，作用于5-HT刺激的磷酸肌醇水解。了解更多

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- Madeleine S A Tan, .et al. Fabrication and Characterization of Clozapine Nanoemulsion Sol-Gel for Intranasal Administration, Mol Pharm, 2022, Sep 23 PMID: 36149013
- Madeleine S. A. Tan, .et al. Clozapine-Encapsulated Binary Mixed Micelles in Thermosensitive Sol-Gels for Intranasal Administration, Gels, 2022, Jan; 8(1): 38 PMID: 35049572
- Milan D Valyear, .et al. Dissociable mesolimbic dopamine circuits control responding triggered by alcohol-predictive discrete cues and contexts, Nat Commun, 2020, Jul 28;11(1):3764 PMID: 32724058
- Yutaro Kobayashi, .et al. Clozapine-dependent inhibition of EGF/neuregulin receptor (ErbB) kinases, Transl Psychiatry, 2019, 9:181 PMID: 31371697
- M.D. Valyear, .et al. Divergent mesolimbic dopamine circuits support alcohol-seeking triggered by discrete cues and contexts, bioRxiv, 2018, 2018
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Flumazenil

Catalog No. A10397
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Benzodiazepine 拮抗剂

Flumazenil是竞争性抑制GABA/苯二氮卓受体复合物上苯二氮卓识别位点的活性。Flumazenil在一些活性动物模型中是弱部分激动剂，但在人类中很少或没有激动剂活性。了解更多

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Amiloride HCl

Catalog No. A10064
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Na+ channel blocker

Amiloride HCl是一种Na+通道阻滞剂，还抑制TRPP3通道和Na+/H+交换剂（NHE）。了解更多

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- Yu Y, .et al. Expression, Localization and Functional Activity of the Major Na+/H+ Exchange Isoforms Expressed in the Intestinal Cell Line Caco-2BBe, Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thomas D. Williams, .et al. The physiological regulation of macropinocytosis during Dictyostelium growth and development, J Cell Sci, 2018, Mar 15; 131(6): jcs213736 PMID: 29440238
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Atazanavir

Catalog No. A10097
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HIV Protease 抑制剂

Atazanavir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。了解更多

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Azacitidine(Vidaza)

Catalog No. A10105
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DNMT 抑制剂

Azacitidine (Vidaza)是DNA和RNA中使用的胞嘧啶核苷的化学类似物，主要用于治疗骨髓增生异常综合症（MDS）。了解更多

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Azathioprine

Catalog No. A10107
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Azathioprine是一种免疫抑制药物，可抑制嘌呤合成和GTP结合蛋白Rac1活化，用于治疗器官移植和自身免疫性疾病。了解更多

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Azelastine HCl (Allergodil)

Catalog No. A10117
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Azelastine HCl (Allergodil)是有效的第二代选择性组胺拮抗剂（组胺-H1-受体拮抗剂）。了解更多

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Aztreonam (Azactam, Cayston)

Catalog No. A10118
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Aztreonam (Azactam,Cayston)是一种合成的单环β-内酰胺抗生素 (一种单bactam)，其细胞核是基于一种从紫罗兰色杆菌中分离出来的更简单的单bactam。了解更多

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- Sreevalli Sharma, .et al. Azaindole Based Potentiator of Antibiotics against Gram-Negative Bacteria, ACS Infect Dis, 2021, Nov 12;7(11):3009-3024 PMID: 34699190
- Pholwat S, .et al. Genotypic antimicrobial resistance assays for use on E. coli isolates and stool specimens, PLoS One, 2019, May 10;14(5):e0216747 PMID: 31075137
- Robert Bucki, .et al. Targeting polyelectrolyte networks in purulent body fluids to modulate bactericidal properties of some antibiotics, Infect Drug Resist, 2018, 11: 77-86 PMID: 29391814
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Oxibendazole

Catalog No. A11654
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Oxibendazole是一种苯并咪唑药物，用于预防马匹和某些家养宠物中的round虫，铜霉菌，线虫，pin虫和肺虫感染。了解更多

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Tioconazole

Catalog No. A11655
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Tioconazole是咪唑类的抗真菌药物，用于治疗真菌或酵母菌引起的感染。了解更多

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Flubendazole (Flutelmium)

Catalog No. A11656
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autophagy inducer

Flubendazole (Flutelmium)是一种驱虫药，用于保护犬猫体内的寄生虫和蠕虫。了解更多

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Pioglitazone (Actos)

Catalog No. A11680
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PPARγ 激动剂

Pioglitazone (Actos)是选择性刺激核受体过氧化物酶体增殖物激活的受体γ（PPAR-γ），并在较小程度上刺激PPAR-α。了解更多

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Acitazanolast

Catalog No. A10034
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Acitazanolast是他扎诺司特和抗过敏药的活性代谢产物。了解更多

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AZD2014 (Vistusertib)

Catalog No. A11303
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mTORC1/2 抑制剂

Vistusertib (AZD2014)是一种新型mTOR抑制剂，无细胞试验中IC50为2.8 nM；对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时，对大多数激酶无或有微弱结合力。了解更多

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- Shuhang Dai, .et al. Calcium/calmodulin-dependent protein kinase kinase 2 mediates pleiotropic effects of epidermal growth factor in cancer cells, Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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Brinzolamide

Catalog No. A11765
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Carbonic anhydrase 抑制剂

Brinzolamide是一种碳酸酐酶抑制剂，IC50为3.19 nM。了解更多

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Azilsartan (TAK-536)

Catalog No. A11775
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AT1 Receptor Blocker

Azilsartan (TAK-536)是一种用于治疗高血压的血管紧张素II受体拮抗剂。了解更多

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BAY 61-3606

Catalog No. A11320
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Syk 抑制剂

BAY 61-3606是一种细胞可渗透的咪唑并嘧啶化合物，可作为Syk酪氨酸激酶活性的有效，ATP竞争性，可逆和高度选择性抑制剂，而对Btk，Fyn，Itk，Lyn和Src无抑制作用。了解更多

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- Ju-Won Jang, .et al. Spleen tyrosine kinase regulates crosstalk of hypoxia-inducible factor-1α and nuclear factor (erythroid-derived2)-like 2 for B cell survival, Int Immunopharmacol, 2021, Mar 21;95:107509 PMID: 33761438
- Sojin Park, .et al. BAFF attenuates oxidative stress-induced cell death by the regulation of mitochondria membrane potential via Syk activation in WiL2-NS B lymphoblasts, Sci Rep, 2020, 10: 11784 PMID: 32678160
- Park S, .et al. Spleen tyrosine kinase-dependent Nrf2 activation regulates oxidative stress-induced cell death in WiL2-NS human B lymphoblasts, Free Radic Res, 2018, Sep 11:1-11 PMID: 30203714
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Ketoconazole

Catalog No. A10498
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P450 抑制剂

ketoconazole作为抗真菌药在结构上类似于咪唑，并干扰真菌细胞膜组成成分麦角甾醇以及某些酶的真菌合成。了解更多

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Ranolazine

Catalog No. A10780
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Ranolazine是部分脂肪酸氧化抑制剂，可将ATP的生产从脂肪酸转变为氧效率更高的碳水化合物氧化。了解更多

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Rosiglitazone (BRL-49653)

Catalog No. A10807
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PPAR 激动剂

Rosiglitazone (BRL-49653)是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。了解更多

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TAK-438 (vonoprazan)

Catalog No. A11239
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potassium-competitive acid Blocker

TAK-438 (vonoprazan)是一种新型的钾竞争酸阻滞剂。了解更多

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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Metolazone

Catalog No. A10584
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Metolazone和其他噻嗪类利尿剂可抑制氯化钠转运体的功能，并防止钠和氯化物以及水离开管腔进入小管细胞。了解更多

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17 alpha-propionate

Catalog No. A10009
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Androgen 拮抗剂

17 alpha-propionate是一种新型的局部和外周选择性雄激素拮抗剂。了解更多

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AZD5363

Catalog No. A11759
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AKT 抑制剂

AZD5363是有效的AKT抑制剂，在体内具有药效学活性，有潜力作为单一疗法或联合用药来治疗一系列实体瘤和血液肿瘤。了解更多

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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Trazodone HCl

Catalog No. A11703
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Trazodone HCl 是一种抗抑郁药，属于5-羟色胺受体拮抗剂和再摄取抑制剂。了解更多

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Terazosin hydrochloride

Catalog No. A11740
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Terazosin hydrochloride是一种选择性α1拮抗剂，用于治疗前列腺肥大(BPH)症状。了解更多

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Cobicistat (GS-9350)

Catalog No. A11277
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CYP3A 抑制剂

Cobicistat (GS-9350)是有效，选择性的细胞色素酶P450 3A (CYP3A)抑制剂，包括重要的cyp3a4亚型。它还抑制肠道转运蛋白，增加几种hiv药物的整体吸收，包括atazanavir、darunavir和tenofovir alafenamide延胡索酸盐。了解更多

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