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XAV-939

XAV-939

产品编号 T1878   CAS 284028-89-3
别名: NVP-XAV939, XAV939

XAV939 通过抑制 tankyrase1/2 显示对 Wnt/β-catenin 介导的转录的选择性抑制。它与 TNKS1 和 TNKS2 的催化 (PARP) 域紧密结合,Kd 分别为 99 和 93 nM

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XAV-939, CAS 284028-89-3
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产品目录号及名称: XAV-939 (T1878)
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纯度: 98%
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生物活性
化学信息
存储 & 溶解度
产品描述 XAV-939 shows the selective inhibition against Wnt/β-catenin-mediated transcription by tankyrase1/2 inhibition (IC50: 11/4 nM in cell-free assays).
靶点活性 TNKS1:11 nM (cell free), TNKS2:4 nM (cell free)
体外活性 Examination of various treatment times (2, 5, 8, 12, 18, 24 and 48 hr) and XAV939 concentrations (0.1, 0.5 or 1.0 μM) revealed a significant reduction of DNA-PKcs protein levels by 8 hours with exposures of either 0.5 μM or 1.0 μM XAV939 [1]. XAV939 blocks TNKS binding at 0.1 μM and blocks PARP1/2 binding at 1 μM. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kd = 0.099 and 0.093 μM, respectively) [2].
体内活性 In contrast to vehicle control (VC), administration of XAV-939 resulted in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice. XAV-939 administration remarkably decreased the infiltration of F4/80+ macrophages and CD3+ T cells in inflamed skin lesions induced by IMQ. Furthermore, reduced neutrophilic infiltrates in microabscesses were observed in the lesional skin treated with XAV-939 compared with VC [3].
细胞实验 XAV939, the recently identified small molecule shown to specifically inhibit PARP activity of tankyrase 1 (and tankyrase 2 at higher concentrations), was used here at much lower concentrations than 3-AB. The tankyrase specific inhibitor XAV939 was solubilized in DMSO at 55°C to a stock concentration of 10mM, which was diluted to a working concentration of 100μM; final concentrations of 0.5μM or 1μM were well within the concentration parameters suggested for cell culture experiments to inhibit tankyrase specifically. Cultures were maintained under these conditions for the duration of the designated time course. Controls were exposed to DMSO alone. Following treatment, cells were lysed and prepared for western blot analysis. Tankyrase 1 and DNA-PKcs protein levels were normalized to the β-actin loading controls and quantified [1].
动物实验 XAV-939, a selective inhibitor of tankyrase (TNKS)-1 and TNKS-2, was injected i.p., at a dose of 1 mg/ml, once a day for seven consecutive days of IMQ treatment (injection volume 100 μl). Control mice were injected with 100 μl 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939 [3].
别名 NVP-XAV939, XAV939
分子量 312.31
分子式 C14H11F3N2OS
CAS No. 284028-89-3

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 6.3 mg/mL (20 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Dregalla RC, et al. Regulatory roles of tankyrase 1 at telomeres and in DNA repair: suppression of T-SCE and stabilization of DNA-PKcs. Aging (Albany NY). 2010 Oct;2(10):691-708. 2. Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-620. 3. Bai J, et al. Epigenetic downregulation of SFRP4 contributes to epidermal hyperplasia in psoriasis. J Immunol. 2015 May 1;194(9):4185-98. doi: 10.4049/jimmunol.1403196. Epub 2015 Mar 30. 4. Geng W, Guo X, Zhang L, et al. Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway[J]. Biomedicine & Pharmacotherapy. 2018 Nov;107:484-494.

文献引用

1. Wu M, Zhang X, Zhang W, et al. Cancer Stem Cell Regulated Phenotypic Plasticity Protects Metastasized Cancer Cells from Ferroptosis. Nature Communications. 2022, 13(1): 1-16. 2. Liu X, Xie P, Hao N, et al. HIF-1–regulated expression of calreticulin promotes breast tumorigenesis and progression through Wnt/β-catenin pathway activation. Proceedings of the National Academy of Sciences. 2021, 118(44) 3. Geng W, Guo X, Zhang L, et al. Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway,Resveratrol inhibits proliferation, migration and invasion of multiple myeloma cells via NEAT1-mediated Wnt/β-catenin signaling pathway. Biomedicine & Pharmacotherapy. 2018 Nov;107:484-494. 4. Li X Y, Shi J, Zhao W, et al. Wnt16 from decidual stromal cells regulates HTR8/SVneo trophoblastic cell function via Akt/β-catenin pathway. Reproduction. 2022, 1(aop).

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 神经元分化化合物库 抗乳腺癌化合物库 DNA 损伤和修复分子库 神经再生化合物库 成骨分子库 Wnt/Hedgehog/Notch 通路化合物库 抗结直肠癌化合物库 抗前列腺癌化合物库 抗卵巢癌化合物库

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剂量换算

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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Keywords

XAV-939 284028-89-3 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin poly ADP ribose polymerase Inhibitor β-catenin NVP-XAV939 XAV939 inhibit Beta catenin XAV 939 inhibitor

 

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