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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 284028-89-3 |
| 是否进口 | 否 |
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| 常用名 | XAV-939 | 英文名 | XAV-939 |
|---|---|---|---|
| CAS号 | 284028-89-3 | 分子量 | 312.310 |
| 密度 | 1.5±0.1 g/cm3 | 沸点 | 429.3oC at 760 mmHg |
| 分子式 | C14H11F3N2OS | 熔点 | N/A |
| MSDS | 中文版 美版 | 闪点 | 213.4oC |
XAV-939 是一种具有选择性的 β-catenin -介导的转录抑制剂和轴蛋白的稳定剂，能够抑制 TNKS1 和 TNKS2 的活性，IC50 值分别为 5 和 2 nM。
Fields of Application :
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.
| CAS Number: | 284028-89-3 |
| Purity: | >98% |
| Molecular Weight: | 312.31 |
| Molecular Formula: | C14H11F3N2OS |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | |
| Chemical Name: | |
| Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
XAV939 is a small molecule and selective Wnt pathway transcription factor β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively. IC50 Value: 11 nM(TNKS1); 4 nM(TNKS2) Target: TMKS1/2; β-catenin in vitro: XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. For the detailed information of XAV-939, the solubility of XAV-939 in water, the solubility of XAV-939 in DMSO, the solubility of XAV-939 in PBS buffer, the animal experiment (test) of XAV-939, the cell expriment (test) of XAV-939, the in vivo, in vitro and clinical trial test of XAV-939, the EC50, IC50,and Affinity of XAV-939, Please contact DC Chemicals.
