XAV-939
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
XAV-939是tankyrase 1/2的小分子抑制剂，IC50值分别为11和4 nM[1]。
XAV-939是作为Wnt/β-catenin途径的抑制剂而被筛选到的。在HEK293细胞中，XAV-939显著抑制Wnt3a刺激的STF活性和β-catenin积累。在SW480细胞中，XAV-939也抑制STF的活性，增加β-catenin的磷酸化。据报道，XAV-939通过抑制tankyrases，从而稳定Axin的水平，进而抑制Wnt信号。XAV-939与tankyrase 1和tankyrase 2的催化结构域紧密结合，Ki值分别为99和93 nM。此外，XAV-939显著抑制β-catenin依赖的DLD-1细胞，而非β-catenin不依赖的RKO细胞的集落形成[1]。
参考文献：
[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.
- 1. Qiyun Shi, Lu Huang, et al."The effects of jiawei Duhuo Jisheng mixture on Wnt/β-catenin signaling pathway in the synovium inflamed by knee osteoarthritis: An in vitro and in vivo experiment." J Ethnopharmacol. 2022 Aug 10;294:115363. PMID: 35551975
- 2. Shan Lin, Qingui Chen, et al."Overexpression of HOXB4 Promotes Protection of Bone Marrow Mesenchymal Stem Cells Against Lipopolysaccharide-Induced Acute Lung Injury Partially Through the Activation of Wnt/β-Catenin Signaling." J Inflamm Res. 2021 Jul 27;14:3637-3649. PMID: 34349541
- 3. 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
- 4. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 312.31 |
| Cas No. | 284028-89-3 |
| Formula | C14H11F3N2OS |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥15.62 mg/mL in DMSO |
| Chemical Name | 2-[4-(trifluoromethyl)phenyl]-1,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidin-4-one |
| SDF | Download SDF |
| Canonical SMILES | C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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. |
|
| 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 | ||||
质量控制和MSDS
- 批次:
化学结构
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