>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

XAV-939

XAV-939 (NVP-XAV939) 通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，无细胞试验中IC50为11 nM/4 nM，调节轴蛋白水平，而对 CRE， NF-κB和TGF-β无作用。

货号：
TK0265
规格：

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	284028-89-3
生物活性	XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
分子式	C14H11F3N2Os
分子量	312.31
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 25 mg/mL (80.05 mM; ultrasonic and warming and heat to 60°C) H2O : < 0.1 mg/mL (insoluble)
体内研究	XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model. XAV-939 (1 mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice.
体外研究	XAV939 also binds to recombinant PARP1, although with a significantly lower binding affinity (Kd=1.2 μM). XAV939 (1 μM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell. XAV939 (0.5 μM, 1.0 μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition. XAV-939 (10 nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells.
文献	暂无相关参考文献
纯度及产品资料	98%

推荐产品