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搜索结果：“MK 1775”

“MK 1775”的搜索结果

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Sitagliptin phosphate monohydrate

Catalog No. A10848
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DDP-4 抑制剂

Sitagliptin phosphate monohydrate是二肽基肽酶-4（DPP-4）类的抗糖尿病（抗高血糖）药物。 DPP-4酶的抑制作用被认为会增加胰高血糖素样肽1（GLP-1），从而抑制胰高血糖素释放，刺激胰岛素释放并降低血糖。了解更多

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MK-5108 (VX-689)

Catalog No. A11410
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Aurora A Kinase 抑制剂

MK-5108，也称为VX-689，是Aurora A激酶ATP结合位点的竞争性抑制剂。了解更多

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- Wei TW, .et al. Aurora A and NF-κB Survival Pathway Drive Chemoresistance in Acute Myeloid Leukemia via the TRAF-Interacting Protein TIFA, Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
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SCH 900776 (MK-8776)

Catalog No. A11167
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Chk1 抑制剂

SCH 900776 (MK-8776)是靶向细胞周期检查点激酶1（Chk1）的药物，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。具有潜在的放射增敏和化学增敏活性。了解更多

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- Hong Yang, .et al. APOBEC3B Improves Response to PD-1 Blockade Through DSBs-ATR-CHK1 Pathway, Research Square, 2022, May 9th
- Motofumi Suzuki, .et al. Radiation-Induced Autophagy in Human Pancreatic Cancer Cells is Critically Dependent on G2 Checkpoint Activation: A Mechanism of Radioresistance in Pancreatic Cancer, Int J Radiat Oncol Biol Phys, 2021, May 25;S0360-3016(21)00361-8 PMID: 34112559
- Min Wu, .et al. FLT3/ITD Cooperates With Rac1 To Modulate The Sensitivity Of Leukemic Cells To Chemotherapeutic Agents Via Regulation Of DNA Repair Pathways, Haematologica, 2019, 104 PMID: 30975911
- Permata TBM, .et al. Base excision repair regulates PD-L1 expression in cancer cells, Oncogene, 2019, Feb 12 PMID: 30755733
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
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Aprepitant (MK-0869)

Catalog No. A10083
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neurokinin-1 receptor 拮抗剂

Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。了解更多

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- Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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MK-8245

Catalog No. A11403
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SCD 抑制剂

MK-8245是肝脏靶向的硬脂酰CoA去饱和酶（SCD）抑制剂。MK-8245可用于治疗糖尿病和血脂异常。了解更多

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- Miyayama Y, .et al. Comparative study on the replication of HCV1b genome between wild type and cell culture adaptive mutant in regard to sensitivities against anti-HCV drugs, Microbiol Immunol, 2019, Dec 19 PMID: 31854467
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MK-2048

Catalog No. A11135
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HIV integrase 抑制剂

MK-2048是第二代整合酶抑制剂，旨在用于抵抗HIV感染。了解更多

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Anacetrapib (MK-0859)

Catalog No. A11084
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CETP 抑制剂

Anacetrapib (MK-0859)是一种有效的，选择性，可逆的rhCETP和突变CETP(C13S)抑制剂，IC50分别为7.9 nM和11.8 nM，提高HDL-C，降低LDL-C，不提高醛固酮和血压。了解更多

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MK-0752

Catalog No. A11194
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Gamma-secretase 抑制剂

MK-0752抑制Notch信号通路，这可能会导致Notch信号通路被过度激活的肿瘤细胞诱导生长停滞和凋亡。了解更多

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Raltegravir (MK-0518)

Catalog No. A10775
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HIV-1 integrase 抑制剂

Raltegravir (MK-0518)靶向整合酶，这是一种HIV酶，可将病毒遗传物质整合到人类染色体中，这是HIV发病机理中的关键步骤。了解更多

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- Michal S Barski, .et al. Structural basis for the inhibition of HTLV-1 integration inferred from cryo-EM deltaretroviral intasome structures, Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
- Lea El Khoury, .et al. Spectrometric and computational studies of the binding of HIV-1 integrase inhibitors to viral DNA extremities, PeerJ Preprints, 2019, 7:e27833v1
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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。了解更多

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BIX 02189

Catalog No. A10151
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MEK 抑制剂

BIX 02189是选择性双重MEK5和ERK5（或BMK1）激酶抑制剂，对于MEK5，ERK5，TGFbR1和其他紧密相关的激酶，IC50值分别为1.5、59、580和> 6200 nM。了解更多

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- Mitsunori Miyazaki, .et al. TSC2/Rheb signaling mediates ERK-dependent regulation of mTORC1 activity in C2C12 myoblasts, FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
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Vorinostat (SAHA)

Catalog No. A10979
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HDAC 抑制剂

Vorinostat (SAHA)是HDAC的抑制剂，抑制脱乙酰和导致双方超乙酰化组蛋白和转录因子的积累。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
- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition, Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
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MK-4827 (Niraparib)

Catalog No. A11026
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PARP 抑制剂

MK-4827 (Niraparib)是一种新型有效的口服生物可利用的PARP-1和PARP-2抑制剂。了解更多

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- 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
- Ann-Katrin Hopp, .et al. Mitochondrial NAD+ Controls Nuclear ARTD1-Induced ADP-Ribosylation, Molecular cell, 2021, Jan 21; 81(2): 340?C354 PMID: 33450210
- 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
- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
- Khalid Hilmi, .et al. CTCF facilitates DNA double-strand break repair by enhancing homologous recombination repair, Sci Adv, 2017, May; 3(5): e1601898 PMID: 28560323
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MK-4827 50mg

Catalog No. A11026-50
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VX-680 (MK-0457, Tozasertib)

Catalog No. A10981
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Aurora Kinase 抑制剂

VX-680 (MK-0457,Tozasertib)是一种有效的选择性Aurora激酶小分子抑制剂。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
- W. Joost Lesterhuis, .et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 PMID: 26193793
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Norfloxacin (Norxacin)

Catalog No. A10652
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Topoisomerase 抑制剂

Norfloxacin(Norxacin)是一种广谱抗生素。了解更多

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Hesperadin

Catalog No. A10448
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Aurora B Kinase 抑制剂

Hesperadin是一种人极光B抑制剂，IC50为40 nM，用于防止底物磷酸化。它显著降低AMPK、Lck、MKK1、MAPKAP-K1、CHK1和PHK的活性，而不抑制MKK1在体内的活性。了解更多

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- Wenbin Ji, .et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases, PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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MK-2206 2HCl

Catalog No. A10003
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AKT 抑制剂

MK-2206 2HCl是Akt1/2/3的高选择性抑制剂，IC50分别为8 nM/12 nM/65 nM。了解更多

Product Citations (17)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- 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
- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. Ultradian rhythms of AKT phosphorylation and gene expression emerge in the absence of the circadian clock components Per1 and Per2, PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. Nystatin Regulates Axonal Extension and Regeneration by Modifying the Levels of Nitric Oxide, Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. Chronic Activation of Gp1 mGluRs Leads to Distinct Refinement of Neural Network Activity Through Non-Canonical p53 and Akt Signaling, eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. Anti-apoptotic activity of human matrix metalloproteinase-2 attenuates diabetes mellitus, Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities, Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells, J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. Constitutive activation of p46JNK2 is indispensable for C/EBPδ induction in the initial stage of adipogenic differentiation, Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. Periostin in tumor microenvironment is associated with poor prognosis and platinum resistance in epithelial ovarian carcinoma, Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. The tumor suppressor p53 guides GluA1 homeostasis through Nedd4-2 during chronic elevation of neuronal activity., J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624
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Ostarine (MK-2866, GTx-024)

Catalog No. A10253
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Androgen Receptor Modulators

Ostarine (MK-2866,GTX-024)是一种雄激素受体调节剂(SARM)。了解更多

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