DYRKs-IN-1 hydrochloride 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 hydrochloride has antitumor activity[1][2].
DYRKs-IN-1 hydrochloride (compound 30) increases the cellular potency against the human colon tumor cell line SW 620 with an EC50 of 27 nM[1]. DYRKs-IN-1 hydrochloride (Example 183) is a potent DYRKs inhibitor[2].
[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. [2]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.