AZ 191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
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描述 | The DYRKs (dual-specificity tyrosine phosphorylation-regulated kinases) are an evolutionarily conserved family of protein kinases that are found within the CMGC group[3].DYRKs contain a characteristic tyrosine-X-tyrosine (Y-X-Y) residue motif in their activation loop. Phosphorylation of the second tyrosine residue is critical for kinase activity[4]. AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM. Using in vitro kinase assays, phospho-specific immunoblot analysis and MS in conjunction with AZ191, DYRK1B phosphorylates CCND1 at Thr(286), not Thr(288), in vitro and in cells. In HEK (human embryonic kidney)-293 and PANC-1 cells (which exhibit DYRK1B amplification) DYRK1B drives Thr(286) phosphorylation and proteasome-dependent turnover of CCND1 and this is abolished by AZ191 or DYRK1B RNAi.[5]. AZ191 inhibited liposarcoma cell growth, decreased cell motility, and induced apoptosis. Moreover, combined AZ191 with doxorubicin demonstrated an increased anti-cancer effect on liposarcoma cells[6]. Mean inhibitory concentrations (EC50) of 0.98 ± 0.08 μM/SC84227, 0.60 ± 0.02 μM/SC97202, 6.26 ± 1.64 μM/SC97208, 0.71 ± 0.019 μM/Harmine and 0.63 ± 0.23 μM/AZ-191 were determined with human cytomegalovirus strain AD169-GFP for the infection of primary human fibroblasts[7]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.64mL 2.33mL 1.16mL |
23.28mL 4.66mL 2.33mL |
CAS号 | 1594092-37-1 |
分子式 | C24H27N7O |
分子量 | 429.517 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(69.85 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |