Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WIKI4 是tankyrase 有效抑制剂,其对TNKS2的IC50值为 26 nM。它有效抑制Wnt/β-catenin 信号传导,其EC50值为 75 nM。它通过抑制TNKS2的酶活性来介导其对Wnt/β-catenin 信号传导的影响。它对 SCLC 细胞具有细胞毒性,其IC50值为 0.02 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 495 | 现货 | ||
10 mg | ¥ 763 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,630 | 现货 | ||
100 mg | ¥ 3,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 568 | 现货 |
产品描述 | WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2). |
靶点活性 | TNKS2:15 nM |
体外活性 | WIKI4 inhibitsWnt/?-catenin signaling in all tested cell lines, including A375, DLD1 colorectal cancer, NALM6 B, U2OS osteosarcoma and hESCs. WIKI4 increases the steady-state abundance of theWnt/?-catenin inhibitory protein, AXIN1 by inhibiting tankyrase activity, and thus preventing the ubiquitylation and degradation of AXIN proteins.[1] |
激酶实验 | Recombinant human wild-type and mutant ALK kinase domain proteins (amino acids 1093–1411) are produced in-house using baculoviral expression, preactivated via autophosphorylation with MgATP, and assayed for kinase activity using a microfluidic mobility shift assay. The reactions contained 1.3 nM wild-type ALK or 0.5 nM mutant ALK (appropriate to produce 15-20% phosphorylation of peptide substrate after 1 h of reaction), 3 μM 5-FAM-KKSRGDYMTMQIG-CONH2), 5 mM MgCl2, and the Km level of ATP in 25 mM Hepes, pH 7.1. The inhibitors are shown to be ATP-competitive from kinetic and crystallographic studies. The Ki values are calculated by fitting the conversion (%) to a competitive inhibition equation. ROS1 enzyme is assayed as described above for ALK, except using 0.25 nM recombinant human ROS1 catalytic domain (amino acids 1883-2347). Kinase inhibitor selectivity is evaluated using a 206-kinase panel. |
分子量 | 521.59 |
分子式 | C29H23N5O3S |
CAS No. | 838818-26-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.14 mg/mL (13.69 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9172 mL | 9.5861 mL | 19.1721 mL | 47.9304 mL |
5 mM | 0.3834 mL | 1.9172 mL | 3.8344 mL | 9.5861 mL | |
10 mM | 0.1917 mL | 0.9586 mL | 1.9172 mL | 4.793 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
WIKI4 838818-26-1 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin poly ADP ribose polymerase WIKI-4 inhibit Inhibitor Beta catenin β-catenin WIKI 4 inhibitor