应用 |
A potent inhibitor of beta-catenin, TNKS1, and TNKS2. |
产品介绍 |
XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录,IC50为11 nM/4 nM,调节轴蛋白水平,但对CRE, NF-κB和TGF-β无作用。 |
备注 |
XAV-939 selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
生化机理 |
XAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.3 μM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells. |
别名 |
XAV 939; 3,5,7,8-四氢-2-[4-(三氟甲基)苯基]-4H-噻喃并[4,3-d]嘧啶-4-酮;XAV939; NVP-XAV 939;3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one |