| 货号 | 17693-1mg |
| 描述 | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.1 It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.2,3 AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.4 This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Becker, W. Emerging role of DYRK family protein kinases as regulators of protein stability in cell cycle control. Cell Cycle 11(18), 3389-3394 (2012). 2.Gao, J.,Zheng, Z.,Rawal, B., et al. Mirk/Dyrk1B, a novel therapeutic target, mediates cell survival in non-small cell lung cancer cells. Cancer Biology and Therapy 8(17), 1671-1679 (2009). 3.Keramati, A.R.,Fathzadeh, M.,Go, G.W., et al. A form of the metabolic syndrome associated with mutations in DYRK1B. New England Journal of Medicine 370(20), 1909-1919 (2014). 4.Ashford, A.L.,Oxley, D.,Kettle, J., et al. A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288). Biochemistry Journal 457(1), 43-56 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 429.5 |
| 分子式 | C24H27N7O |
| CAS号 | 1594092-37-1 |
| 稳定性 | ≥ 2 years |
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