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PIK-93

Catalog No. A10731
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PI3K 抑制剂

PIK-93是第一个有效的，人工合成的PI4K(PI4KIIIβ)抑制剂，IC50为19 nM；抑制PI3Kα，IC50为39 nM。了解更多

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- Gavin Ka Yu Siu, .et al. Hepatitis C virus NS5A protein cooperates with phosphatidylinositol 4-kinase IIIα to induce mitochondrial fragmentation, Sci Rep, 2016, 6: 23464 PMID: 27010100
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CP-724714

Catalog No. A10242
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HER2/ErbB2 抑制剂

CP-724714是一种有效的，选择性HER2/ErbB2抑制剂，可抑制HER2激酶（IC50 3.8 ng/ml）。了解更多

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- Yu Muta, .et al. Composite regulation of ERK activity dynamics underlying tumour-specific traits in the intestine, Nat Commun, 2018, 9: 2174 PMID: 29872037
- Gina M. Sizemore, .et al. Stromal PTEN determines mammary epithelial response to radiotherapy, Nat Commun, 2018, 9: 2783 PMID: 30018330
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BMS 599626 (AC480)

Catalog No. A11209
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EGFR 抑制剂

BMS 599626 (AC480)是一种选择性的，高效效的HER1，HER2和HER4酪氨酸激酶抑制剂（IC50分别为22、32和190 nM），具有潜在的抗肿瘤活性。了解更多

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Arry-380 analog

Catalog No. A11027
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HER2 抑制剂

Arry-380 analog是一种ErbB-2抑制剂，可选择性结合并抑制ErbB-2的磷酸化，从而导致表达ErbB-2的肿瘤细胞的生长抑制和死亡。了解更多

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AV-412

Catalog No. A11028
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EGFR 抑制剂

AV-412是一种EGFR / HER2抑制剂，可与表皮生长因子受体（EGFR）和人表皮生长因子受体2（HER2）结合并抑制其生长，这可能会导致肿瘤生长和血管生成受到抑制。了解更多

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- Le Zhang, .et al. High-throughput drug library screening identifies colchicine as a thyroid cancer inhibitor, Oncotarget, 2016, Apr 12; 7(15): 19948-19959 PMID: 26942566
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Bibf1120 (Nintedanib)

Catalog No. A10137
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VEGFR 抑制剂

Bibf1120 (Nintedanib)是一种新型的三联血管激酶抑制剂，可同时抑制三种生长因子受体：VEGFR，PDGF和FGFR。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
- Chun-Jung Chang, .et al. Overcoming interferon (IFN)-γ resistance ameliorates transforming growth factor (TGF)-β-mediated lung fibroblast-to-myofibroblast transition and bleomycin-induced pulmonary fibrosis, Biochem Pharmacol, 2021, Jan;183:114356 PMID: 33285108
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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

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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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PP242 (Torkinib)

Catalog No. A10746
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mTOR 抑制剂

PP242 (Torkinib)在mTORC1和mTORC2中都是有效的选择性mTOR抑制剂。了解更多

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- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
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AZ628

Catalog No. A11063
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Raf 抑制剂

AZ628是一种RAF抑制剂，IC50值：BRAF V600E和野生型CRAF约为30 nM，野生型BRAF约为100 nM。了解更多

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YM201636

Catalog No. A11064
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PI3K 抑制剂

YM201636是PIKfyve的细胞渗透性和选择性抑制剂（IC50 = 33 nM）。了解更多

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- Krishna Chintaluri, .et al. The PH domain from the Toxoplasma gondii PH-containing protein-1 (TgPH1) serves as an ectopic reporter of phosphatidylinositol 3-phosphate in mammalian cells, PLoS One, 2018, 13(6): e0198454 PMID: 29870544
- Dayam RM, .et al. The Lipid Kinase PIKfyve Coordinates the Neutrophil Immune Response through the Activation of the Rac GTPase, J Immunol, 2017, Sep 15;199(6):2096-2105 PMID: 28779020
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AG-490

Catalog No. A10047
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EGFR 抑制剂

AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。了解更多

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- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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SGI-1776 (free base)

Catalog No. A10838
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PIM1 抑制剂

SGI-1776 (free base)是Pim1的一种新型ATP竞争性抑制剂，在无细胞试验中的IC50为7 nM，选择性是Pim2和Pim3的50倍和10倍，对Flt3和haspin也有效。阶段1。了解更多

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- Ishikawa C, .et al. Expression and significance of Pim-3 kinase in adult T-cell leukemia, Eur J Haematol, 2017, Dec;99(6):495-504 PMID: 28833639
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AEE788

Catalog No. A10043
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EGFR 抑制剂

AEE788是一种口服生物可用的多受体酪氨酸激酶抑制剂，可抑制EGFR，HER2和VEGF2酪氨酸激酶的磷酸化。了解更多

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Palomid 529 (P529)

Catalog No. A10693
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AKT 抑制剂

Palomid 529是PI3K/Akt/mTOR途径的双重TORC1/2抑制剂，在血管生成和细胞增殖中具有广泛的活性。了解更多

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GSK690693

Catalog No. A11030
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AKT 抑制剂

GSK690693是一种新型的ATP竞争性低纳摩尔泛Akt激酶抑制剂（IC50值分别为Akt1、2和3的2、13和9 nM）。了解更多

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- Khan MI, .et al. Thalidomide attenuates development of m0rphine dependence in mice by inhibiting PI3K/Akt and nitric oxide signaling pathways, Prog Neuropsychopharmacol Biol Psychiatry, 2018, Mar 2;82:39-48 PMID: 9223784
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AT7867

Catalog No. A10094
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AKT 抑制剂

AT7867是AKT和下游激酶p70 S6激酶（p70S6K）以及蛋白激酶A的新型有效抑制剂。了解更多

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CCT128930

Catalog No. A11031
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AKT 抑制剂

CCT128930是一种具有ATP竞争性的AKT抑制剂，是一种有效的高级吡咯并嘧啶铅化合物，相对于PKA表现出对AKT的选择性，可通过靶向单个氨基酸差异实现。了解更多

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PHT-427

Catalog No. A11032
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AKT 抑制剂

PHT-427是一种新型的Akt/磷脂酰肌醇依赖性蛋白激酶1 pleckstrin同源域抑制剂。了解更多

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Triciribine phosphate (NSC-280594)

Catalog No. A11033
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AKT 抑制剂

Triciribine phosphate是一种DNA synthesis抑制剂，也抑制PC3细胞系中的Akt和CEM-SS，H9，H9IIIB，U1细胞中的HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000 了解更多

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A-674563

Catalog No. A11034
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Akt 抑制剂

A-674563是一种B/Akt抑制剂，IC50为14 nM，并且还显示出对PKA和CDK2的抑制活性，IC50分别为16和46 nM。了解更多

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- Kobayashi T, .et al. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells, Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. Pre-clinical assessment of A-674563 as an anti-melanoma agent, Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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SU11274

Catalog No. A10869
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c-Met 抑制剂

SU11274是一种Met酪氨酸激酶抑制剂。了解更多

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PHA-665752

Catalog No. A10713
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c-Met 抑制剂

PHA665752是c-Met/HGF/SF信号传导的小分子抑制剂。了解更多

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SGX-523

Catalog No. A10839
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c-Met 抑制剂

SGX-523是一种口服生物可利用的小分子，与c-Met蛋白或HGFR特异性结合，可防止HGF结合并破坏MET信号通路。了解更多

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JNJ-38877605

Catalog No. A10493
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c-Met 抑制剂

JNJ-38877605是一种ATP竞争性的c-Met抑制剂，从而抑制c-Met磷酸化并破坏c-Met信号转导途径。了解更多

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BMS-777607

Catalog No. A10153
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c-Met 抑制剂

BMS-777607是一种MET酪氨酸激酶抑制剂，与c-Met蛋白或HGFR结合，可防止HGF结合并破坏MET信号通路。了解更多

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MGCD-265 (Glesatinib)

Catalog No. A10587
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c-Met 抑制剂

MGCD-265 (Glesatinib)是一种多靶酪氨酸激酶抑制剂，可与多种RTK（包括c-Met受体（HGFR）结合并抑制其磷酸化。Tek/Tie-2受体；VEGFR类型1、2和3；和MST1R。了解更多

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PF-04217903

Catalog No. A10711
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c-Met 抑制剂

PF-04217903是一种选择性的，ATP竞争性c-Met抑制剂，在A549细胞中IC50为4.8 nM，对致癌基因突变型敏感(对Y1230C突变型没有活性)。了解更多

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AMG 208

Catalog No. A10063
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c-Met 抑制剂

AMG 208是一种新型c-Met抑制剂，可抑制c-Met的配体依赖性和配体依赖性活化，从而抑制其酪氨酸激酶活性。了解更多

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Roscovitine (Seliciclib)

Catalog No. A10806
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CDK 抑制剂

Roscovitine (Seliciclib)是一种CDK抑制剂，可优先抑制多种酶靶标，包括CDK2，CDK7和CDK9。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
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MGCD0103 (Mocetinostat)

Catalog No. A10586
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HDAC 抑制剂

MGCD0103 (Mocetinostat)是一种苯甲酰胺组蛋白脱乙酰基酶抑制剂，主要抑制组蛋白脱乙酰基酶1（HDAC1），但也抑制HDAC2，HDAC3和HDAC11。了解更多

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- Mari Ishigami-Yuasa, .et al. Class IIb HDAC Inhibition Enhances the Inhibitory Effect of Am80, a Synthetic Retinoid, in Prostate Cancer, Biol Pharm Bull, 2019, 42, 448-452
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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Imiquimod (Aldara)

Catalog No. A10469
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TLR7 激动剂

Imiquimod (Aldara)是一种杂环咪唑并喹啉酰胺，用作免疫反应调节剂。了解更多

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- 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
- Kunishita Y, .et al. TRIM21 Dysfunction Enhances Aberrant B-Cell Differentiation in Autoimmune Pathogenesis, Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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PD173074

Catalog No. A10703
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FGFR1/VEGFR2 抑制剂

PD173074是有效的，细胞可渗透的和ATP竞争性的FGFR和VEGFR抑制剂。了解更多

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- Cheryl Q.E. Lee, .et al. What Is Trophoblast? A Combination of Criteria Define Human First-Trimester Trophoblast, Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
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KU-55933

Catalog No. A10506
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ATM 抑制剂

KU-55933是ATM抑制剂，通过抑制细胞增殖，并通过阻断Akt过度激活的癌细胞中的Akt诱导凋亡。了解更多

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- Mariko Shikata, .et al. 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Histone Acetylation via α7nAChR-Mediated PI3K/Akt Activation and Its Impact on γ-H2AX Generation, Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. Combination Therapy with Reovirus and ATM Inhibitor Enhances Cell Death and Virus Replication in Canine Melanoma, Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a γH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D, Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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Rolipram

Catalog No. A10805
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PDE4 抑制剂

Rolipram是一种PDE4抑制剂，IC50 = 2.0μM。了解更多

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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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GSK2126458 (Omipalisib)

Catalog No. A11035
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mTOR/PI3K 抑制剂,

GSK2126458 (Omipalisib)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。了解更多

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LY2603618 (IC-83)

Catalog No. A11036
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Chk 抑制剂

LY2603618 (IC-83)是一种chk2抑制剂，可与chk2结合并抑制其活性，这可能会阻止DNA损伤剂引起的DNA修复。了解更多

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- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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VX-765 (Belnacasan)

Catalog No. A10984
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Caspase-1/4 抑制剂

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。了解更多

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- Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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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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ITF2357 (Givinostat)

Catalog No. A10488
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HDAC 抑制剂

ITF2357 (Givinostat)是一种HDACS抑制剂，具有潜在的抗炎、抗血管生成和抗肿瘤活性。了解更多

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Droxinostat

Catalog No. A10337
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HDAC 抑制剂

Droxinostat是HDAC3，HDAC6和HDAC8的选择性抑制剂，显示出可比较的HDAC6和HDAC8抑制作用，IC50分别为2.47和1.46μmol/ L。了解更多

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AR-42 (HDAC-42)

Catalog No. A11037
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HDAC 抑制剂

AR-42 (HDAC-42)是一种新型的HDAC抑制剂，通过下调本构激活的Kit表现出对恶性肥大细胞系的生物学活性。了解更多

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- Yong-Hui Liao, .et al. Histone deacetylase 2 is involved in μ-opioid receptor suppression in the spinal dorsal horn in a rat model of chronic pancreatitis pain, Mol Med Rep, 2018, Feb; 17(2): 2803-2810 PMID: 29257262
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SB590885

Catalog No. A10829
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B-Raf 抑制剂

SB590885是B-Raf激酶的选择性小分子抑制剂，B-Raf和c-Raf的Ki app值分别为0.16和1.72 nM。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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Moxifloxacin HCl

Catalog No. A10609
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Topoisomerase 抑制剂

Moxifloxacin HCl是一种喹诺酮/氟喹诺酮类抗菌剂。了解更多

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- Hiroshi Arakawa, .et al. Possible interaction of quinolone antibiotics with peptide transporter 1 in oral absorption of peptide-mimetic drugs, Biopharm Drug Dispos, 2016, Jan;37(1):39-45 PMID: 26590007
- Arisa Higa, .et al. Differing responses of human stem cell-derived cardiomyocytes to arrhythmogenic drugs, determined using impedance measurements, Fundam. Toxicol. Sci, 2016, 3(2): 47-53
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Tandutinib (MLN518)

Catalog No. A10887
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FLT3 抑制剂

Tandutinib (MLN518)是一种有效的FLT3抑制剂，c-KIT和PDGF受体酪氨酸激酶的自磷酸化，从而抑制细胞增殖并诱导细胞凋亡。了解更多

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SB 203580

Catalog No. A10824
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p38 MAPK 抑制剂

SB 203580是p38α和p38β的特异性抑制剂，可抑制MAPKAP激酶2和热激蛋白27的下游激活。了解更多

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- Lei Zhang, .et al. Ripk3 signaling regulates HSCs during stress and represses radiation-induced leukemia in mice, Stem Cell Reports, 2022, Jun 14;17(6):1428-1441 PMID: 35561683
- Tomoyuki Hashimoto, .et al. Development of radioiodinated pyrimidinopyridone derivatives as targeted imaging probes of activated p38α for single photon emission computed tomography, Ann Nucl Med, 2021, Aug 19 PMID: 34410619
- Y Zou, .et al. Autophagy inhibition enhances Matrine derivative MASM induced apoptosis in cancer cells via a mechanism involving reactive oxygen species-mediated PI3K/Akt/mTOR and Erk/p38 signaling, BMC Cancer, 2019, Oct 15;19(1):949 PMID: 31615459
- Wei P, .et al. Transforming growth factor (TGF)-β1-induced miR-133a inhibits myofibroblast differentiation and pulmonary fibrosis, Cell Death Dis, 2019, Sep 11;10(9):670 PMID: 31511493
- Uwada J, .et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells, Cell Signal, 2019, Nov;63:109358 PMID: 31295519
- 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
- Uwada J, .et al. Activation of muscarinic receptors prevents TNF-α-mediated intestinal epithelial barrier disruption through p38 MAPK, Cell Signal, 2017, Jul;35:188-196 PMID: 28412413
- ZHIQIANG ZHANG, .et al. Tumor necrosis factor-like weak inducer of apoptosis regulates particle-induced inflammatory osteolysis via the p38 mitogen-activated protein kinase signaling pathway., Mol Med Rep. , 2015, Jul;12(1):1499-505. PMID: 25815691
- 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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SB 431542

Catalog No. A10826
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TGF-beta/Smad 抑制剂

SB 431542是转化生长因子-β超家族I型激活素受体样激酶（ALK）受体ALK4，ALK5和ALK7的有效抑制剂。了解更多

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- Huong Pham, .et al. BMP11 Negatively Regulates Lipid Metabolism in C2C12 Muscle Cells, Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. Obesity Reduces Mammary Epithelial Cell TGFβ1 Activity Through Macrophage-Mediated Extracellular Matrix Remodeling, FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
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WYE-125132 (WYE-132)

Catalog No. A11038
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mTOR 抑制剂

WYE-125132 (WYE-132)是一种高度有效的，ATP竞争性的mTOR抑制剂，IC50为0.19 nM；作用于mTOR比作用于PI3Ks或PI3K相关激酶hSMG1和ATR选择性高。了解更多

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MLN8054

Catalog No. A10601
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Aurora A 抑制剂

MLN8054是一种有效的，选择性Aurora A抑制剂，在Sf9昆虫细胞中IC50为4 nM，作用于Aurora A比作用于Aurora B选择性高40倍，可在体内和体外诱导人肿瘤细胞衰老。了解更多

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