| 应用 |
An ATP-competitive CK2 protein kinase inhibitor. |
| 产品介绍 |
CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。 |
| 备注 |
CX-4945 is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1. |
| 生化机理 |
CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase 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 anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 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 causes cell-cycle arrest and selectively induced apoptosis in certain cancer 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. |
| 别名 |
CX-4945; CX 4945; CX4945; 5-[(3-氯苯基)氨基]苯并[c]-2,6-萘啶-8-羧酸;Silmitasertib;CX 4945;CX4945; 5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylic acid |
