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別名: NVP-XAV939
XAV-939 (NVP-XAV939) 通過抑制tankyrase1/2而選擇性抑制Wnt/β-catenin介導的轉(zhuǎn)錄,無細胞試驗中IC50為11 nM/4 nM,調(diào)節(jié)軸蛋白水平,而對 CRE, NF-κB和TGF-β無作用。
XAV-939 Chemical Structure
CAS: 284028-89-3
Bocchicchio S, et al. J Cell Physiol. 2019 Dec;234(12):22130-22143.
相關(guān)靶點 | PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2 | 點擊展開 |
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相關(guān)產(chǎn)品 | Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide | 點擊展開 |
相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 干細胞小分子化合物庫 GPCR小分子化合物庫 干細胞分化化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | XAV-939 (NVP-XAV939) 通過抑制tankyrase1/2而選擇性抑制Wnt/β-catenin介導的轉(zhuǎn)錄,無細胞試驗中IC50為11 nM/4 nM,調(diào)節(jié)軸蛋白水平,而對 CRE, NF-κB和TGF-β無作用。 | ||||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | XAV939 是小分子選擇性抑制劑,抑制Wnt通路轉(zhuǎn)錄因子β-catenin調(diào)節(jié)的轉(zhuǎn)錄,作用于TNKS1和TNKS2時IC50分別為11和4nM。XAV939通過穩(wěn)定axin和斷裂混合物的極限濃度組成促進β-catenin降解, 而穩(wěn)定axin是通過阻斷PAR酶:端錨聚合酶1和2 。2種端錨聚合酶亞型因為axin的高度保守區(qū)而相互作用,促進了端錨聚合酶通過泛素-蛋白酶體途徑的降解。XAV939抑制Wnt/β-catenin通路活性已經(jīng)用于多種癌癥治療。[1] XAV939尤其抑制端錨聚合酶PARP活性。XAV939 明顯降低DNA-PKcs蛋白水平, 說明了在維持DNA-PKcs蛋白穩(wěn)定性時端錨聚合酶PARP活性的關(guān)鍵性。用1.0 μM XAV939處理12小時,DNA-PKcs蛋白水平降低到最低水平,與用DMSO處理的對照組相比,相對表達量小于25%。1.0 μM XAV939治療人類成淋巴細胞,導致端錨聚合酶1水平明顯上升。[2] |
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細胞實驗 | 細胞系 | WTK1成淋巴細胞 | ||
濃度 | 1.0 μM | |||
孵育時間 | 8小時 | |||
方法 | XAV939溶解在DMSO中,儲存濃度為10mM, 實驗處理時稀釋到100 μM。實驗組,用1.0 μM XAV939處理WTK1成淋巴細胞8小時,對照組用DMSO處理,上樣到4-20%梯度SDS-PAGE孔中。2小時上樣一次。在0, 2,和4 小時分別上樣,結(jié)果分別跑膠2, 4,和6小時。最后,通過western blot分析。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 |
分子量 | 312.31 | 分子式 | C14H11F3N2OS |
CAS號 | 284028-89-3 | SDF | Download XAV-939 SDF |
Smiles | C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 12 mg/mL ( (38.42 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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問題 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.