Description
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor and has antitumor activity.
Uses
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity[1][2].
in vitro
From a data-mining effort, the team has discovered analogues of pyrido[2,3-d]pyrimidines as potent enantio-selective inhibitors of DYRK1B. Cells treated with a tool compound from this series showed the same cellular effects as down regulation of DYRK1B with siRNA._x000D_
_x000D_
Reference: Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. https://pubmed.ncbi.nlm.nih.gov/24239188/
target
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively.
IC 50
DYRK1A: 5 nM (IC50); DYRK1B: 8 nM (IC50)
References
[1] Anderson K, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. DOI:
10.1016/j.bmcl.2013.10.055[2] Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.
