| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| X408951-1ml |
1ml |
现货  |
|
| 英文别名 | NVP-XAV939 | 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | XAV-939 |
| 生化机理 | XAV-939（NVP-XAV939）通过抑制tankyrase1/2选择性地抑制Wnt/β-catenin介导的转录，在无细胞实验中的IC50为11 nM/4 nM，可调节轴突蛋白水平，但不影响CRE、NF-κB或TGF-β。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
XAV-939通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，IC50为11 nM/4 nM，调节轴蛋白水平，但对CRE， NF-κB和TGF-β无作用。A potent inhibitor of beta-catenin, TNKS1, and TNKS2. Information XAV-939 XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin -mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. 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. In vivo
cell lines：L6 cell lines Concentrations：1.0 μM Incubation Time：8 hours Powder Purity:≥98% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F |
| PubChem CID | 135418940 |
| 分子量 | 312.31 |
| 象形图 | GHS06, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H319: 引起严重眼睛刺激 H301: 吞咽会中毒 |
| 预防措施声明 |
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 |
| WGK Germany | 3 |
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