XAV939；NVP-XAV 939

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抑制剂描述：

产品名称：XAV-939

产品别名：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

英文别名：XAV939;NVP-XAV 939

靶点：TNKS1；TNKS2；ARTD2；ARTD1

CAS：284028-89-3

纯度：>98%

外观：白色至浅黄色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：

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.

溶解性：DMSO ：6.3 mg/mL (20 mM)

体外研究：

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.

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.

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