XAV-939
别名: NVP-XAV939
XAV-939 (NVP-XAV939) 通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，无细胞试验中IC50为11 nM/4 nM，调节轴蛋白水平，而对 CRE， NF-κB和TGF-β无作用。
XAV-939 Chemical Structure
CAS: 284028-89-3
产品质控
批次：
纯度：
99.95%
99.95
常与XAV-939一起在实验中被使用的化合物
XAV-939促进前中枢神经系统的同一性，而SU5402则加速hPSC向神经外胚层谱系的分化。
XAV-939和LDN-193189在不同程度上改善低密度P0 RPE培养物的形态方面效果最差。
XAV939和ICG-001降低IGROV1和SKOV3卵巢癌细胞系的增殖。
Bocchicchio S, et al. J Cell Physiol. 2019 Dec;234(12):22130-22143.
XAV-939相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| SW480 | Function Assay | 10 μM | 24 h | Stabilization of Axin2 with EC50 of 0.371 μM | 22260203 |
| Sf-21 | Kinase Assay | 18.75 μM | 60 min | Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM | 23879431 |
| DLD1 | Function Assay | 20 μM | 24 h | Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity | 24527792 |
| DLD1 | Cytotoxic Assay | 20 μM | 10 d | Cytotoxicity assessed as growth inhibition | 24527792 |
| HeLa | Function Assay | 10 μM | 48 h | Reduction of cytoplasmic distribution and nuclear translocation of β-catenin | 25061499 |
| SiHa | Function Assay | 10 μM | 48 h | Reduction of cytoplasmic distribution and nuclear translocation of β-catenin | 25061499 |
| HEK293T | Function Assay | 50 μM | Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE | 22260203 | |
| HEK293T | Function Assay | 10 μM | Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM | 22191557 | |
| VERO | Function Assay | 25 μM | Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion | 25332845 | |
| IEC-6 | Function Assay | 6 h | Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced lgr5 expression with IC50 of 2.9 μM | 24060489 | |
| IEC-6 | Function Assay | 6 h | Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced axin2 expression with IC50 of 0.64 μM | 24060489 | |
| HEK293T | Function Assay | 24 h | Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM | 22260203 | |
| DLD1 | Function assay | 24 hrs | Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay, IC50 = 0.707 μM. | 25299683 | |
| Sf21 | Function assay | 2 hrs | Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins, IC50 = 0.017 μM. | 27163581 | |
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 12.3 μM. | 29934219 | |
| HEK293T | Function Assay | Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM | 23879431 | ||
| HEK293 | Function assay | Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50 = 0.078 μM. | 23844574 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | XAV-939 (NVP-XAV939) 通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，无细胞试验中IC50为11 nM/4 nM，调节轴蛋白水平，而对 CRE， NF-κB和TGF-β无作用。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | XAV939 是小分子选择性抑制剂，抑制Wnt通路转录因子β-catenin调节的转录，作用于TNKS1和TNKS2时IC50分别为11和4nM。XAV939通过稳定axin和断裂混合物的极限浓度组成促进β-catenin降解， 而稳定axin是通过阻断PAR酶：端锚聚合酶1和2 。2种端锚聚合酶亚型因为axin的高度保守区而相互作用，促进了端锚聚合酶通过泛素-蛋白酶体途径的降解。XAV939抑制Wnt/β-catenin通路活性已经用于多种癌症治疗。[1] XAV939尤其抑制端锚聚合酶PARP活性。XAV939 明显降低DNA-PKcs蛋白水平, 说明了在维持DNA-PKcs蛋白稳定性时端锚聚合酶PARP活性的关键性。用1.0 μM XAV939处理12小时，DNA-PKcs蛋白水平降低到最低水平，与用DMSO处理的对照组相比，相对表达量小于25%。1.0 μM XAV939治疗人类成淋巴细胞，导致端锚聚合酶1水平明显上升。[2] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | WTK1成淋巴细胞 | ||
| 浓度 | 1.0 μM | |||
| 孵育时间 | 8小时 | |||
| 方法 | XAV939溶解在DMSO中，储存浓度为10mM, 实验处理时稀释到100 μM。实验组，用1.0 μM XAV939处理WTK1成淋巴细胞8小时，对照组用DMSO处理，上样到4-20%梯度SDS-PAGE孔中。2小时上样一次。在0, 2，和4 小时分别上样，结果分别跑胶2, 4，和6小时。最后，通过western blot分析。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | β-catenin / E-cadherin / N-cadherin β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin |
|
31060551 | |
| Immunofluorescence | β-catenin / E-cadherin Actin / PAR Hes1 / β-catenin / p-STAT3 |
|
31060551 | |
化学信息&溶解度
| 分子量 | 312.31 | 分子式 | C14H11F3N2OS |
| CAS号 | 284028-89-3 | SDF | Download XAV-939 SDF |
| Smiles | C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 12 mg/mL ( (38.42 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.
回答：
S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.
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