产品描述
| 溶解性 | Soluble in 1:5 EtOH:PBS (pH 7.2) (~0.15 mg/ml), DMSO (~2 mg/ml), DMF (~5 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C. |
| 存贮条件 | 储存温度-20°C |
| 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 |
