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MAPK

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GSK1120212 (JTP-74057, Trametinib)

Catalog No. A11029
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MEK 抑制剂

GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。了解更多

Product Citations (10)

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- Nao Yamagishi, .et al. Non-canonical Regulation of EGFR by the Air Pollutant 9,10-Phenanthrenequinone, Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
- Hayato Mizuta, .et al. Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer, Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Keisuke Yanagida, .et al. Sphingosine 1-Phosphate Receptor Signaling Establishes AP-1 Gradients to Allow for Retinal Endothelial Cell Specialization, Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Kanemaru Y, .et al. Dramatic response of BRAF V600E-mutant epithelioid glioblastoma to combination therapy with BRAF and MEK inhibitor: establishment and xenograft of a cell line to predict clinical efficacy, Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
- Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
- Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
- Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- 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
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
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PD98059

Catalog No. A10705
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MEK 抑制剂

PD98059是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。了解更多

Product Citations (9)

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- Anna Nakanishi, .et al. Effects of human induced pluripotent stem cell-derived intestinal organoids on colitis-model mice, Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Isamu Ogawa, .et al. Suspension culture of human induced pluripotent stem cell-derived intestinal organoids using natural polysaccharides, Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Akinobu Nakamura, .et al. Engineering Orthogonal, Plasma Membrane-Specific SLIPT Systems for Multiplexed Chemical Control of Signaling Pathways in Living Single Cells, ACS Chem Biol, 2020, Apr 17;15(4):1004-1015 PMID: 32162909
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Kwang Woon Kim, .et al. Dual-Targeting AKT2 and ERK in cancer stem-like cells in neuroblastoma, Oncotarget, 2019, Sep 24; 10(54): 5645-5659 PMID: 31608140
- Tsai CC, .et al. Protease-activated receptor 2 induces migration and promotes Slug-mediated epithelial-mesenchymal transition in lung adenocarcinoma cells, Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Kim MH, .et al. C16?ceramide and sphingosine 1?phosphate/S1PR2 have opposite effects on cell growth through mTOR signaling pathway regulation, Oncol Rep, 2018, Nov;40(5):2977-2987 PMID: 30226616
- Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
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AZD6244 (Selumetinib)

Catalog No. A10257
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MEK 抑制剂

Selumetinib (AZD6244)是一种有效，高选择性的MEK抑制剂，ARRY142886，AZD-6244和ARRY-142886是MEK 1/2抑制剂，GI50值在14至50 nm之间。了解更多

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- Chia-Chi Chang, .et al. Upregulation of lactate dehydrogenase a by 14-3-3ζ leads to increased glycolysis critical for breast cancer initiation and progression, Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
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MEK162 (ARRY-438162, Binimetinib)

Catalog No. A11493
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MEK1/2 抑制剂

MEK162 (ARRY-438162,Binimetinib)是MEK1/2的一种强效、选择性ATP非竞争性抑制剂。了解更多

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- S Shahab, .et al. MEK Inhibition Suppresses Growth of Atypical Teratoid/Rhabdoid Tumors, J Neuropathol Exp Neurol, 2020, Jul 1;79(7):746-753
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
- Alquezar C, .et al. Increasing progranulin levels and blockade of the ERK1/2 pathway: Upstream and downstream strategies for the treatment of progranulin deficient frontotemporal dementia, Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
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U0126-EtOH

Catalog No. A10957
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MEK 抑制剂

U0126-EtOH是MEK1和MEK2的抑制剂，IC50分别为72 nM和58 nM。了解更多

Product Citations (4)

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- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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PD0325901

Catalog No. A10256
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MEK 抑制剂

PD0325901是一种选择性的，非ATP竞争性MEK抑制剂，无细胞试验中IC50为0.33 nM，对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。了解更多

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- Jan Langkabel, .et al. Induction of peri-implantation stage synthetic embryos using reprogramming paradigms in ESCs, bioRxiv, 2021, January 25
- Ryan Clarke, .et al. Sequential Activation of Guide RNAs to Enable Successive CRISPR-Cas9 Activities, Mol Cell, 2021, Jan 21;81(2):226-238.e5 PMID: 33378644
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fukumoto S, .et al. Synergistic anti-proliferative effects of mTOR and MEK inhibitors in high-grade chondrosarcoma cell line OUMS-27, Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960
- Yoshiteru Yano, .et al. Non-neural and cardiac differentiating properties of Tbx6-expressing mouse embryonic stem cells, Regenerative Therapy, 2016, 3 (2016) 1-6
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GDC-0973 (Cobimetinib)

Catalog No. A11441
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MEK1 抑制剂

GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂，IC50为4.2 nM，对MEK1的选择性选择性是对MEK2的100倍以上，并且当针对一组超过100个丝氨酸的抑制剂进行测试时，没有显示出明显的抑制作用。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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BI-847325

Catalog No. A15762
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MEK/Aurora 抑制剂

BI-847325是一种生物利用型选择性MEK/Aurora双重激酶抑制剂，对于非洲爪蟾Aurora B，人Aurora A和Aurora C以及IC50分别为3 nM，25 nM，15 nM，25 nM和4 nM IC50人MEK1和MEK2。了解更多

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- Hilda Samimi, .et al. Alginate-based 3D cell culture technique to evaluate the half-maximal inhibitory concentration: an in vitro model of anticancer drug study for anaplastic thyroid carcinoma, Thyroid Res, 2021, Dec 3;14(1):27 PMID: 34861882
- Hilda Samimi, .et al. Transcript-level regulation of MALAT1-mediated cell cycle and apoptosis genes using dual MEK/Aurora kinase inhibitor "BI-847325" on anaplastic thyroid carcinoma, DARU J Pharm Sci, 2019, 1-7 PMID: 31077090
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Refametinib (RDEA-119, BAY 86-9766)

Catalog No. A12866
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MEK1/2 抑制剂

Refametinib (RDEA-119,BAY 86-9766)是一种口服生物利用型选择性MEK抑制剂，EC50为 2.0-15 nM。具有潜在的抗肿瘤活性。了解更多

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- Estelle Daudigeos-Dubus, etc. Regorafenib: Antitumor Activity upon Mono and Combination Therapy in Preclinical Pediatric Malignancy Models. PLoS One. 2015; 10(11): e0142612.
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Cobimetinib (racemate)

Catalog No. A15050
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MEK 抑制剂

Cobimetinib (racemate)是一种有效的，高度选择性的MEK1/2抑制剂。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Chun-Yu Liu, .et al. Varlitinib Downregulates HER/ERK Signaling and Induces Apoptosis in Triple Negative Breast Cancer Cells, Cancers (Basel), 2019, Jan 17;11(1) PMID: 30658422
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Refametinib

Catalog No. A11264
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MEK 抑制剂

Refametinib是一种有效的，ATP非竞争性和高度选择性的MEK1和MEK2抑制剂，IC50分别为19 nM和47 nM。了解更多

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GDC-0623

Catalog No. A12974
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MEK1 抑制剂

GDC-0623是一种有效的ATP竞争性MEK1抑制剂，Ki为0.13 nM。了解更多

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PD 198306

Catalog No. A16032
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MEK 抑制剂

PD 198306是一种有效的，选择性的和非ATP竞争性MAPK/ERK激酶（MEK）抑制剂。了解更多

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SL-327

Catalog No. A14137
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MKK/MEK 抑制剂

SL-327是MEK1和MEK2的选择性抑制剂（IC50值分别为0.18和0.22μM）；在体外阻断海马LTP。全身性给药后，体内的脑渗透剂会阻止大鼠的恐惧条件和学习，并在小鼠中产生神经保护作用。了解更多

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G-479

Catalog No. A14380
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MEK 抑制剂

G-479是有效的MEK抑制剂。在许多方面，极性分布在整个分子中的G-479被证明具有比GDC-0623更高的生物活性。了解更多

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Cobimetinib (R-enantiomer)

Catalog No. A15051
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MEK 抑制剂

Cobimetinib R-enantiomer是Cobimetinib的R对映异构体，Cobimetinib是一种有力的，高选择性的促分裂原活化蛋白激酶（MEK1/2）抑制剂。了解更多

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PD 334581

Catalog No. A16044
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MEK1 抑制剂

PD 334581在生物学研究中用于评估卤素键合，作为合理药物设计的新型相互作用。它也是MEK1的抑制剂。了解更多

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RO4927350

Catalog No. A11247
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MEK1/2 抑制剂

RO4927350是一种有效且高度选择性的非ATP竞争性MEK1/2抑制剂。了解更多

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AS703026 (Pimasertib)

Catalog No. A10089
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MEK1/2 抑制剂

AS703026 (Pimasertib)是一种新型的，选择性的，口服可生物利用的MEK1/2抑制剂，可抑制MM细胞的生长和存活以及细胞因子诱导的破骨细胞分化。了解更多

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RO4987655

Catalog No. A13272
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MEK1 抑制剂

RO4987655是一种口服活性小分子，靶向有丝分裂原激活的蛋白激酶激酶1（MAP2K1或MEK1），抑制 MEK1/MEK2，IC50 为 5.2 nM。具有潜在的抗肿瘤活性。了解更多

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PD184352 (CI-1040)

Catalog No. A10212
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MEK1/2 抑制剂

PD184352 (CI-1040)是一种ATP非竞争性MEK1/2抑制剂，在基于细胞的测定中，IC50为17 nM，对MEK1/2的选择性是对MEK5的100倍。了解更多

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- Sachio Suzuki, .et al. A chemogenetic platform for controlling plasma membrane signaling and synthetic signal oscillation, Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. Synthetic Protein Condensates That Inducibly Recruit and Release Protein Activity in Living Cells, J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
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AZD8330

Catalog No. A10115
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MEK 抑制剂

AZD8330是新型，选择性，非ATP竞争性MEK 1/2抑制剂，IC50为7 nM。阶段1。了解更多

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PD318088

Catalog No. A10704
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MEK 抑制剂

PD318088是MEK1和MEK2的抑制剂。了解更多

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RO5126766 (CH5126766)

Catalog No. A14019
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Raf/MEK dual 抑制剂

RO5126766 (CH5126766)是对Raf和MEK丝裂原激活的蛋白激酶（MAPK）具有特异性的蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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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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