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XAV-939

现货
Catalog No.
A1877
Tankyrase 1/2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
5mg
¥ 500.00
现货
25mg
¥ 1,200.00
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100mg
¥ 3,000.00
现货

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Background

XAV-939 is a small-molecule inhibitor of tankyrase 1/2 with IC50 values of 4 and 11 nM, respectively [1].

XAV-939 was screened out as an inhibitor of Wnt/β-catenin pathway. In HEK293 cells, XAV-939 significantly inhibited the Wnt3a-stimulated STF activity and β-catenin accumulation. In SW480 cells, XAV-939 also inhibited STF activity and increased β-catenin phosphorylation. XAV-939 was demonstrated to stabilize the axin levels through inhibiting tankyrases and subsequently inhibit the Wnt signaling. It tightly bound to the catalytic domains of tankyrase 1 and tankyrase 2 with Kd values of 99 and 93 nM, respectively. In addition, XAV-939 significantly inhibited colony formation of β-catenin-dependent DLD-1 cells but not β-catenin-independent RKO cells [1].

References:
[1] Huang S M A, Mishina Y M, Liu S, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature, 2009, 461(7264): 614-620.

文献引用

1. Grunewald ME, Chen Y, et al. "The coronavirus macrodomain is required to prevent PARP-mediated inhibition of virus replication and enhancement of IFN expression." PLoS Pathog. 2019 May 16;15(5):e1007756. PMID:31095648
2. Jia J, Qiao Y, et al."Tankyrase inhibitors suppress hepatocellular carcinoma cell growth via modulating the Hippo cascade." PLoS One. 2017 Sep 6;12(9):e0184068. PMID:28877210

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt312.31
Cas No.284028-89-3
FormulaC14H11F3N2OS
Solubility≥15.62mg/mL in DMSO
Chemical Name2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one
SDFDownload SDF
Canonical SMILESC1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HCT116 细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

20 μM,24小时

实验结果

使用XAV-939处理HCT116细胞,然后用PI染色并进行流式细胞术分析或裂解进行免疫印迹分析。结果显示,阻滞在G1期的细胞数为71.01%,而未处理对照组样品为45.54%。蛋白质印迹分析结果显示,XAV-939增加AXIN的水平并抑制β-连环蛋白的表达。

动物实验[2]:

动物模型

小鼠

剂量

腹膜内注射, 2.5 mg/kg, 每天四次

实验结果

与假处理的bleomycin攻击小鼠相比,使用XAV-939治疗bleomycin攻击的小鼠减少50%的真皮增厚。在用XAV-939处理的小鼠中,肌成纤维细胞的数量和羟脯氨酸含量也显著降低。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] He L, Lu N, Dai Q, et al. Wogonin induced G1 cell cycle arrest by regulating Wnt/β-catenin signaling pathway and inactivating CDK8 in human colorectal cancer carcinoma cells. Toxicology, 2013, 312: 36-47.

[2] Distler A, Deloch L, Huang J, et al. Inactivation of tankyrases reduces experimental fibrosis by inhibiting canonical Wntsignalling. Annals of the rheumatic diseases, 2013, 72(9): 1575-1580.

生物活性

XAV-939是TNKS1和TNKS2的抑制剂,IC50值分别为11和4 nM。.
靶点 TNKS1 TNKS2        
IC50 11 nM 4 nM        

质量控制

化学结构

XAV-939

相关生物数据

XAV-939

相关生物数据

XAV-939

相关生物数据

XAV-939

相关生物数据

XAV-939