现货,CX-4945 ,CAS号:1009820-21-6,美国进口,TGF-beta / smad , PKC ,PKC 抑制剂,selleck,S2248

信号转导通路: TGF-beta / smad >> PKC >> PKC 抑制剂 >> CX-4945http://selleck.cn/cx-4945-S2248.html

技术数据:

分子量(MW): 349.77

化学式:

C19H12ClN3O2

 

溶解度: DMSO ≥70mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1009820-21-6

生物活性

 

 

CX-4945 is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad spectrum anti-proliferative activity in multiple cancer cell lines. The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 (CX 4945; Silmitasertib) was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo. [1][2][3]

 

 

 

参考文献

CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy Denis Drygin, Nicole Streiner, et al. Cancer Res 2010;70:10288-10298

Structural basis of CX-4945 binding to human protein kinase CK2 Andrew D. Ferguson, Payal R. Sheth,et al. FEBS Letters 2011;585:104–110

Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the Treatment of Cancer Fabrice Pierre,PeterC.Chua,et al. J. Med. Chem 2011;54:635–654

 

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