Pricing updated 2019-06-15. Prices are subject to change without notice.
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.4
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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).
Gao, J., Zheng, Z., Rawal, B., et al. Mirk/Dyrk1B, a novel therapeutic target, mediates cell survival in non-
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).