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搜索结果：“2c c hcl”

“2c c hcl”的搜索结果

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LY317615 (Enzastaurin)

Catalog No. A10356
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PKCβ 抑制剂

LY317615（Enzastaurin）是一种有效的，选择性的PKCβ抑制剂，具有抗增殖活性（IC50 =?6 nM）。了解更多

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VX-702

Catalog No. A10982
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p38 MAPK 抑制剂

VX-702是一种高选择性p38α MAPK抑制剂，可抑制血小板激动剂诱导的p38激活（IC50 = 4至20 nM）。了解更多

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- Wei-Chun HuangFu, etc. Inflammatory signaling compromises cell responses to interferon alpha. Oncogene. 2012 Jan 12; 31(2): 161–172.
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SB939 ( Pracinostat )

Catalog No. A10830
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HDAC 抑制剂

SB939 (Pracinostat)是HDAC的口服抑制剂，对I，II和IV类HDAC具有选择性，在体外HDAC1活性测定中显示IC50值为77 nM。了解更多

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- 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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Sclareolide (Norambreinolide)

Catalog No. A10832
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Sclareolide (Norambreinolide)是一种倍半萜内酯天然产物，来源于各种植物，包括Salvia sclarea，Salvia yosgadensis，和 cigar tobacco。了解更多

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XAV 939

Catalog No. A10994
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PARP 抑制剂

XAV 939是TNKS抑制剂（TNKS1和TNKS2的IC50值分别为0.011和0.004μM）。了解更多

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- Shizu Aikawa, .et al. Autotaxin-lysophosphatidic acid-LPA 3 signaling at the embryo-epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- 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
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BMS-794833

Catalog No. A10154
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c-Met 抑制剂

BMS-794833是Met和VEGFR-2的有效ATP竞争性抑制剂，IC50为1.7和15 nM。了解更多

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AMG-458

Catalog No. A11055
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c-Met 抑制剂

AMG-458是一种有效的c-Met抑制剂，IC50值为60nM，对VEGFR2具有选择性。了解更多

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Ispinesib (SB-715992)

Catalog No. A10486
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KSP 抑制剂

Ispinesib (SB-715992)是驱动蛋白纺锤体蛋白的有效抑制剂，驱动蛋白纺锤体蛋白是双极有丝分裂纺锤体形成和有丝分裂细胞周期进程所必需的驱动蛋白。了解更多

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JNJ-26481585 (Quisinostat)

Catalog No. A10492
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HDAC 抑制剂

JNJ-26481585 (Quisinostat)是一种pan-HDAC抑制剂，对HDAC1具有显著的效力(IC(50)，0.16 nmol/L)。了解更多

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- Minoru Ueda, .et al. The Distinct Roles of Class I and II RPD3-Like Histone Deacetylases in Salinity Stress Response, Plant Physiol, 2017, Dec; 175(4): 1760-1773 PMID: 29018096
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S3I-201 (NSC 74859)

Catalog No. A10817
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Stat3 抑制剂

S3I-201(NSC 74859)是Stat3的新型抑制剂，可在体外抑制Stat3，Stat3复合物的形成以及Stat3-DNA结合活性（IC50 = 86±33 ?M）和Stat3依赖性转录活性。了解更多

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- Bae WJ, .et al. PTPRD-inactivation-induced CXCL8 promotes angiogenesis and metastasis in gastric cancer and is inhibited. J Exp Clin Cancer Res, 2019, 38:484 PMID: 31805999
- Nishimura K, .et al. Effect of erythropoietin production induced by hypoxia on autophagy in HepG2 cells, Biochem Biophys Res Commun, 2018, Jan 1;495(1):1317-1321 PMID: 29191652
- Ethan L. Morgan, .et al. STAT3 activation by E6 is essential for the differentiation-dependent HPV18 life cycle, PLoS Pathog, 2018, Apr; 14(4): e1006975 PMID: 29630659
- Soleimani AH, .et al. Micellar nano-carriers for the delivery of STAT3 dimerization inhibitors to melanoma, Drug Deliv Transl Res, 2017, Aug;7(4):571-581 PMID: 28290050
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VX-745

Catalog No. A10983
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p38 MAPK 抑制剂

VX-745是一种有效的，选择性p38α抑制剂，IC50为10 nM，比作用于p38β选择性高22倍，对p38γ没有抑制作用。了解更多

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Candesartan (Atacand)

Catalog No. A10175
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RAAS 拮抗剂

Candesartan (Atacand)是一种血管紧张素受体阻滞剂（也称为血管紧张素II受体拮抗剂或AIIRA）。了解更多

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- Hideki Kobara, .et al. Antihypertensive drug telmisartan inhibits cell proliferation of gastrointestinal stromal tumor cells in vitro, Molecular Medicine Reports, 2020, 22(2)
- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
- Toshihide Kashihara, .et al. Angiotensin II activates CaV1.2 Ca2+ channels through β‐arrestin2 and casein kinase 2 in mouse immature cardiomyocytes, J Physiol, 2017, Jul 1; 595(13): 4207-4225 PMID: 28295363
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Linifanib (ABT-869)

Catalog No. A10025
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VEGFR/PDGFR 抑制剂

Linifanib (ABT-869)是一种结构新颖的有效RTK，VEGF和PDGF抑制剂，对人内皮细胞，PDGFR-β，KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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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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Cidofovir (Vistide)

Catalog No. A10214
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DNA/RNA Synthesis 抑制剂

Cidofovir (Vistide)通过选择性抑制病毒DNA的合成而抑制病毒复制。了解更多

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- Adhikary A, .et al. π-Radical to σ-Radical Tautomerization in One-Electron-Oxidized 1-Methylcytosine and Its Analogs, J Phys Chem B, 2015, Sep 3;119(35):11496-505 PMID: 26237072
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Marbofloxacin

Catalog No. A10557
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Topoisomerase 抑制剂

Marbofloxacin是有效的第三代氟喹诺酮类抗生素，通过抑制细菌DNA复制起作用。了解更多

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OSI-027

Catalog No. A11056
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mTOR 抑制剂

OSI-027是一种有效的，选择性的，可口服生物利用的mTOR激酶抑制剂，可抑制与mTOR的TORC1和TORC2复合物相关的激酶活性。了解更多

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Vatalanib (PTK787) 2HCl

Catalog No. A10967
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VEGFR 抑制剂

Vatalanib (PTK787) 2HCl是一种小分子蛋白激酶抑制剂，可抑制抑制所有已知VEGF受体以及血小板衍生的生长因子受体β和c-kit的血管生成，但对VEGFR-2的选择性最高。了解更多

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Abiraterone (CB-7598)

Catalog No. A10020
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CYP17 抑制剂

Abiraterone (CB-7598)是一种有效CYP17抑制剂，20裂合酶（CYP17A1）。了解更多

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Abiraterone Acetate (CB7630)

Catalog No. A11058
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CYP17 抑制剂

Abiraterone Acetate是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂。了解更多

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Hexestrol

Catalog No. A10451
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Estrogen/progestogen Receptor 激动剂

Hexestrol是一种致癌的合成雌激素，可抑制微管聚合和带状结构的形成。它是脂质过氧化的抑制剂。了解更多

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Docetaxel (Taxotere)

Catalog No. A10326
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Microtubule Associated 抑制剂

Docetaxel (Taxotere)多西他赛一种taxol类似物，是一种microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。了解更多

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Paclitaxel (Taxol)

Catalog No. A10689
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Microtubule Associated 抑制剂

Paclitaxel (Taxol)是一种有丝分裂抑制剂，可稳定微管，从而干扰细胞分裂过程中微管的正常分解，在人内皮细胞中IC50为0.1pM。了解更多

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- Yu Pan, .et al. The nature of the modification at position 37 of tRNAPhe correlates with acquired taxol resistance, Nucleic Acids Res, 2021, Jan 11;49(1):38-52 PMID: 33290562
- Li-Li Li, .et al. Resonance energy transfer sensitises and monitors in situ switching of LOV2-based optogenetic actuators, Nat Commun, 2020, Oct 9;11(1):5107 PMID: 33037199
- Baglo Y, .et al. Harnessing the Potential Synergistic Interplay Between Photosensitizer Dark Toxicity and Chemotherapy, Photochem Photobiol, 2019, Dec 19 PMID: 31856423
- Owiti AO, .et al. PSMA Antibody-Conjugated Pentablock Copolymer Nanomicellar Formulation for Targeted Delivery to Prostate Cancer, AAPS PharmSciTech, 2018, Nov;19(8):3534-3549 PMID: 30151731
- Owiti AO, .et al. Strategic Pentablock Copolymer Nanomicellar Formulation for Paclitaxel Delivery System, AAPS PharmSciTech, 2018, Oct;19(7):3110-3122 PMID: 30112614
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Vincristine sulfate

Catalog No. A10973
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Tubulin 抑制剂

Vincristine sulfate是一种有丝分裂抑制剂。了解更多

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Epothilone A

Catalog No. A10359
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Microtubule Associated 抑制剂

Epothilone A 通过稳定紫杉醇结合位点处的微管形成而起作用，并导致细胞周期停滞在G2/M转变，从而导致细胞毒性。了解更多

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Epothilone B (EPO906)

Catalog No. A10360
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Microtubule Associated 抑制剂

Epothilone B (EPO906)是一种紫杉醇样microtubule稳定剂。了解更多

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- Yicheng Zhu, .et al. Combinatrial treatment of anti-High Mobility Group Box-1 monoclonal antibody and epothilone B improves functional recovery after spinal cord contusion injury, Neurosci Res, 2021, Apr 17 PMID: 33864880
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Vinflunine Tartrate

Catalog No. A10975
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Microtubule Associated 抑制剂

Vinflunine Tartrate是长春氟宁的酒石酸盐，它使微管不稳定，IC50为18.8 nM，并在细胞分裂过程中干扰微管的动力学。了解更多

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Dasatinib (BMS-354825)

Catalog No. A10290
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Abl-Src 抑制剂

Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL，Src，c-Kit，ephrin受体和其他几种酪氨酸激酶，但不是erbB激酶，例如EGFR或Her2。了解更多

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- Chihiro Motozono, .et al. The SARS-CoV-2 Omicron BA.1 spike G446S mutation potentiates antiviral T-cell recognition, Nat Commun, 2022, Sep 21;13(1):5440 PMID: 36130929
- 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
- David E J Klawon, .et al. Altered selection on a single self-ligand promotes susceptibility to organ-specific T cell infiltration, J Exp Med, 2021, Jun 7;218(6) PMID: 33914024
- 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
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Sano T, .et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 PMID: 30121259
- Ines Peschel, .et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 PMID: 28522571
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- John D. Leonard, .et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8 PMID: 28709804
- 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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Pimobendan (Vetmedin)

Catalog No. A10733
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PDE 抑制剂

Pimobendan (Vetmedin)是一种钙增敏剂，具有正性肌力和血管舒张作用。它也是磷酸二酯酶III（PDE3）的选择性抑制剂。了解更多

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CX-4945 (Silmitasertib)

Catalog No. A11060
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CK2 抑制剂

CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，可抑制人脐静脉内皮细胞迁移，管形成，并阻止癌细胞中CK2依赖性缺氧诱导的因子1α（HIF-1α）转录。了解更多

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- Xixi Zhao, .et al. Phosphorylation and Stabilization of PD-L1 by CK2 Suppresses Dendritic Cell Function, Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines, Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells, Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. Protein kinase CK2 impact on intracellular calcium homeostasis in prostate cancer, Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. Protein kinase CK2 is involved in zinc homeostasis in breast and prostate cancer cells, Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. Human Rad17?C-terminal tail is phosphorylated by concerted action of CK1δ/ε and CK2 to promote interaction with the 9-1-1 complex, Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. Casein kinase 2 promotes interaction between Rad17 and the 9-1-1 complex through constitutive phosphorylation of the C-terminal tail of human Rad17, Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. Casein kinase 2 controls the survival of normal thymic and leukemic γδ T cells via promotion of AKT signaling, Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly, Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. Protein Kinase CK2 Regulates Leukocyte-Endothelial Cell Interactions during Ischemia and Reperfusion in Striated Skin Muscle, Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. Role of protein kinase CK2 in the dynamic interaction of platelets, leukocytes and endothelial cells during thrombus formation., Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. Inhibition of protein kinase CK2 suppresses tumor necrosis factor (TNF)-α-induced leukocyte-endothelial cell interaction., Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. Adult B-cell acute lymphoblastic leukemia cells display decreased PTEN activity and constitutive hyperactivation of PI3K/Akt pathway despite high PTEN protein levels, Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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ENMD-2076

Catalog No. A10352
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Aurora A / FLT3 抑制剂

ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。了解更多

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Ki16425

Catalog No. A10501
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LPA Receptor 拮抗剂

ki16425是对LPA1和LPA3具有选择性的LPA受体拮抗剂，对人LPA1、LPA2和LPA3受体分别显示Ki值为0.34、6.5和0.93 μM。了解更多

Product Citations (5)

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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. Lateral access mechanism of LPA receptor probed by molecular dynamics simulation, PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6, Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. Generalized pruritus in primary sclerosing cholangitis: implications of histamine release by lysophosphatidic acid., Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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Curcumol

Catalog No. A10247
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JAK2 抑制剂

Curcumol是常见的传统中药，具有抗肿瘤活性。了解更多

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Taxifolin

Catalog No. A10893
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VEGFR-2 抑制剂

Taxifolin以很大的结合能值结合在VEGFR-2激酶的ATP结合位点上，并起I型竞争性抑制剂的作用。了解更多

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- Keji Yu, .et al. A role for ascorbate conjugates of (+)-catechin in proanthocyanidin polymerization, Nat Commun, 2022, Jun 14;13(1):3425 PMID: 35701431
- Shinji Kondo, .et al. Antidiabetic Effect of Taxifolin in Cultured L6 Myotubes and Type 2 Diabetic Model KK-Ay/Ta Mice with Hyperglycemia and Hyperuricemia, Curr Issues Mol Biol, 2021, Sep 26;43(3):1293-1306 PMID: 34698101
- Shin-ichi Adachi, .et al. Anti-hyperuricemic effect of taxifolin in cultured hepatocytes and model mice, Cytotechnology, 2017, Apr; 69(2): 329-336 PMID: 28101741
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TW-37

Catalog No. A10955
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Bcl-2 抑制剂

TW-37是Bcl-2的小分子抑制剂，可抑制胰腺癌细胞的生长，并通过一种涉及Notch-1和Jagged-1失活的新途径介导的胰腺癌细胞凋亡。了解更多

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Andarine (GTX-007)

Catalog No. A10076
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Androgen Receptor 激动剂

Andarine (GTX-007)是研究性的选择性雄激素受体调节剂（SARM）。了解更多

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Glycyrrhetinic acid (Enoxolone)

Catalog No. A10353
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15-PGDH 抑制剂

Glycyrrhetinic acid (Enoxolone)是一种通过甘草酸水解得到的β-香树脂醇型五环三萜衍生物。了解更多

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SB 216763

Catalog No. A10825
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GSK-3 抑制剂

SB 216763是一种有效且具有选择性的细胞渗透性ATP竞争性GSK3α抑制剂，IC50值为34 nM（与GSK3β相似的效力）。了解更多

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SB 415286

Catalog No. A11061
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GSK-3 抑制剂

SB 415286是一种有效且具有选择性的细胞渗透性ATP竞争性GSK3α抑制剂，IC50值为78 nM（与GSK3β相似的效价），Ki值为31 nM。了解更多

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CX-5461

Catalog No. A11065
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DNA/RNA Synthesis 抑制剂

CX-5461是RNA聚合酶I（Pol I）的一流的非遗传毒性小分子靶向抑制剂，可激活p53途径而不会引起DNA损伤。了解更多

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- Taro Mannena, .et al. Distinct RNA polymerase transcripts direct the assembly of phase-separated DBC1 nuclear bodies in different cell lines, Mol Biol Cell, 2021, 32:ar33, 1?C11 PMID: 34495685
- Shuichiro Okamoto, .et al. The rRNA synthesis inhibitor CX-5461 may induce autophagy that inhibits anticancer drug-induced cell damage to leukemia cells, Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
- Ahmed Abdullah Ahmed, .et al. A G-quadruplex-binding compound shows potent activity in human gemcitabine-resistant pancreatic cancer cells, Sci Rep, 2020, 10: 12192 PMID: 32699225
- Abed Saady, .et al. Applying styryl quinolinium fluorescent probes for imaging of ribosomal RNA in living cells, Dyes Pigm, 2020, 174: 107986
- Jackobel AJ, .et al. DNA binding preferences of S. cerevisiae RNA polymerase I Core Factor reveal a preference for the GC-minor groove and a conserved binding mechanism, Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
- Hiroaki Suzuki, .et al. The proline-arginine repeat protein linked to C9-ALS/FTD causes neuronal toxicity by inhibiting the DEAD-box RNA helicase-mediated ribosome biogenesi, Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
- Anastasia Gelgor, .et al. Nucleolar stress enhances lytic reactivation of the Kaposi??s sarcoma-associated herpesvirus, Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
- Wang ZF, .et al. The Hairpin Form of r(G4C2)exp in c9ALS/FTD Is Repeat-Associated Non-ATG Translated and a Target for Bioactive Small Molecules, Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
- Yuko Fujiwara, .et al. A Nucleolar Stress-Specific p53-miR-101 Molecular Circuit Functions as an Intrinsic Tumor-Suppressor Network, EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
- Maïmouna Coura Kone, .et al. Three-Dimensional Distribution of UBF and Nopp140 in Relationship to Ribosomal DNA Transcription During Mouse Preimplantation Development, Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997
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AMG 900

Catalog No. A11066
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Aurora Kinase 抑制剂

AMG 900是一种新型有效且高度选择性的泛Aurora激酶抑制剂，在紫杉烷抗性肿瘤细胞系中具有活性。了解更多

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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
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TAK-901

Catalog No. A11067
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Aurora Kinase A/B 抑制剂

TAK-901是一种新型Aurora A/B抑制剂，IC50为21 nM/15 nM。它不是细胞JAK2，c-Src或Abl的有效抑制剂。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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PF-562271

Catalog No. A11192
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FAK 抑制剂

PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。了解更多

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- Jiping Yue, .et al. In vivo epidermal migration requires focal adhesion targeting of ACF7, Nat Commun, 2016, 7: 11692 PMID: 27216888
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A-769662

Catalog No. A11071
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AMPK 激活剂

A-769662是AMP激活的蛋白激酶（AMPK）的新激活剂。了解更多

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- Daniel Missailidis, .et al. Dysregulated Provision of Oxidisable Substrates to the Mitochondria in ME/CFS Lymphoblasts, Int J Mol Sci., 2021, Feb; 22(4): 2046 PMID: 33669532
- Lieberthal W, .et al. AMPK-mediated activation of Akt protects renal tubular cells from stress-induced apoptosis in vitro and ameliorates ischemic AKI in vivo, Am J Physiol Renal Physiol, 2019, 2019 PMID: 30995114
- Kikuchi H, .et al. Failure to sense energy depletion may be a novel therapeutic target in chronic kidney disease, Kidney Int, 2018, Nov 13. pii: S0085-2538(18)30635-5 PMID: 30455054
- Schneider H, .et al. AMPK Dilates Resistance Arteries via Activation of SERCA and BKCa Channels in Smooth Muscle, Hypertension, 2015, Jul;66(1):108-16 PMID: 26034200
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GSK1904529A

Catalog No. A10440
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IGF-1R 抑制剂

GSK1904529A分别用27和25 nmol/L的IC(50)s选择性抑制IGF-IR和IR。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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JTC-801

Catalog No. A11076
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Opioid Receptor 拮抗剂

JTC-801是nociceptin receptor（也称为ORL-1受体）的选择性拮抗剂。了解更多

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- Lihao Gu, .et al. 10-Hydroxy-2-Decenoic Acid in Royal Jelly Extract Induced Both Filaggrin and Amino Acid in a Cultured Human Three-Dimensional Epidermis Model, Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. Brain opioid and nociceptin receptors are involved in regulation of bombesin-induced activation of central sympatho-adrenomedullary outflow in the rat, Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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ZM 336372

Catalog No. A11077
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C-Raf 抑制剂

ZM 336372是有效的ATP Raf-1体外竞争性抑制剂 (IC50 = 70 nM)。了解更多

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