store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT251545 是一种有效的、具有口服活性的WNT 抑制剂,在 7dF3 细胞中对 WNT 抑制作用的IC50值为 5 nM。它是选择性化学探针,用于探索 CDK8 和 CDK19 在人类疾病中的作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 536 | 现货 | ||
2 mg | ¥ 779 | 现货 | ||
5 mg | ¥ 1,430 | 现货 | ||
10 mg | ¥ 2,420 | 现货 | ||
25 mg | ¥ 3,970 | 现货 | ||
50 mg | ¥ 5,830 | 现货 | ||
100 mg | ¥ 7,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 932 | 现货 |
产品描述 | CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells). |
靶点活性 | WNT (7dF3 cells):5 nM |
体外活性 | CCT251545, a small-molecule inhibitor of the WNT pathway discovered through cell-based screening, is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.?X-ray crystallography demonstrates a type 1 binding mode involving insertion of the CDK8 C terminus into the ligand binding site.?In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity.?We show that CCT251545 and close analogs alter WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.?Consistent with this, we find that phosphorylation of STAT1(SER727) is a biomarker of CDK8 kinase activity in vitro and in vivo[1]. |
体内活性 | In vivo, CCT251545 with WNT-dependent tumors activity[1]. |
分子量 | 421.92 |
分子式 | C23H24ClN5O |
CAS No. | 1661839-45-7 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45mg/ml (106.66 Mm)
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。
CCT251545 1661839-45-7 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin inhibit Wnt Inhibitor CCT 251545 CCT-251545 inhibitor