Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZ191 是特异性 DYRK1B 抑制剂。它对 DYRK1B 的特异性分别是 DYRK1A 和 DYRK2 的 5 倍和 110 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 392 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 877 | 现货 | ||
25 mg | ¥ 1,470 | 现货 | ||
50 mg | ¥ 2,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively. |
靶点活性 | DYRK1B:17 nM |
体外活性 | AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression. [1] |
激酶实验 | Biochemical Binding Affinity – HTRF Assay: The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient. |
分子量 | 429.52 |
分子式 | C24H27N7O |
CAS No. | 1594092-37-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 1 mg/mL (2.32 mM)
DMSO: 79 mg/mL (183.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.3282 mL | 11.6409 mL | 23.2818 mL | 58.2045 mL |
DMSO | 5 mM | 0.4656 mL | 2.3282 mL | 4.6564 mL | 11.6409 mL |
10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL | 5.8205 mL | |
20 mM | 0.1164 mL | 0.582 mL | 1.1641 mL | 2.9102 mL | |
50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.1641 mL | |
100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.582 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。
AZ191 1594092-37-1 Cell Cycle/Checkpoint Tyrosine Kinase/Adaptors DYRK Inhibitor Dual specificity tyrosine regulated kinase Dual specificity tyrosine phosphorylation regulated kinase inhibit AZ 191 AZ-191 inhibitor