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Onalespib (AT13387)

Catalog No. A11062
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HSP90 抑制剂

Onalespib (AT13387)是Hsp90的靶向抑制剂，可抑制其伴侣功能并促进涉及肿瘤细胞增殖和存活的致癌信号蛋白的降解。了解更多

Product Citations (3)

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- Boucherat O, .et al. Mitochondrial HSP90 Accumulation Promotes Vascular Remodeling in Pulmonary Arterial Hypertension, Am J Respir Crit Care Med, 2018, Jul 1;198(1):90-103 PMID: 29394093
- Olivier Boucherat, .et al. HDAC6: A Novel Histone Deacetylase Implicated in Pulmonary Arterial Hypertension, Sci Rep, 2017, 7: 4546 PMID: 28674407
- Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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OSI-420

Catalog No. A10678
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EGFR 抑制剂

OSI-420 (Desmethyl Erlotinib,CP-473420)是一种口服活性EGFR酪氨酸激酶抑制剂，可通过抑制细胞间结构域来抑制受体酪氨酸激酶（TKs）。了解更多

Product Citations (2)

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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade, Breast Cancer Res, 2017, 19: 90 PMID: 28778177
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CUDC-101

Catalog No. A10246
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HDAC 抑制剂

CUDC-101是一种抑制多种靶标的新型化合物，旨在抑制HDAC，EGFR和Her2。了解更多

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BSI-201 (Iniparib)

Catalog No. A10164
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PARP 抑制剂

BSI-201 (Iniparib)是一种有效的PARP-1抑制剂，已被证明可以穿越血脑屏障。了解更多

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- 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
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AG-014699 (Rucaparib)

Catalog No. A10045
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PARP 抑制剂

AG-014699 (Rucaparib)是一种PARP抑制剂，可抑制聚（ADP-核糖）聚合酶（PARP，后者是DNA修复中的关键酶。无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。了解更多

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- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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AG14361

Catalog No. A10046
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PARP 抑制剂

AG14361是一种有效的PARP抑制剂，可在MMR（错配修复）有效/不足的细胞中增强替莫唑胺（TMZ）的细胞毒性。了解更多

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- 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
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A-966492

Catalog No. A10019
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PARP1 抑制剂

A-966492在全细胞试验中显示出对K（i）为1 nM，EC（50）为1 nM的聚（ADP-核糖）聚合酶-1（PARP-1）酶的高效力。了解更多

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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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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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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

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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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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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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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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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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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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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

Product Citations (7)

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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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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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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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ICG-001

Catalog No. A11039
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Wnt/beta-catenin 抑制剂

ICG-001是Wnt/β-catenin信号传导途径的特异性抑制剂，可抑制β-catenin/环状AMP响应元件结合（CREB）蛋白的转录（IC50 = 3 uM）。了解更多

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- Seonmin Choi, .et al. Indocyanine Green-Loaded PLGA Nanoparticles Conjugated with Hyaluronic Acid Improve Target Specificity in Cervical Cancer Tumors, Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. Cardiac function and feed efficiency: increased right-heart workload in feed inefficient beef cattle, Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. Small Heterodimer Partner Controls the Virus-Mediated Antiviral Immune Response by Targeting CREB-Binding Protein in the Nucleus, Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. CD90 expression in human intrahepatic cholangiocarcinoma is associated with lymph node metastasis and poor prognosis, J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. Wnt3a promotes differentiation of human bone marrow-derived mesenchymal stem cells into cementoblast-like cells, In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
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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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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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Baicalin

Catalog No. A10121
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HIV-1 production 抑制剂

Baicalin是已知的脯氨酰内肽酶抑制剂，并且影响GABA受体。了解更多

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- Shoichi Ozawa, .et al. Uremic serum residue decreases SN-38 sensitivity through suppression of organic anion transporter polypeptide 2B1 in LS-180 colon cancer cells, Sci Rep, 2019, 9: 15464

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