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DYRKs-IN-1 hydrochloride

Names

[ CAS No. ]:
1386980-55-7

[ Name ]:
DYRKs-IN-1 hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK

[Target]

DYRK1A:5 nM (IC50)

DYRK1B:8 nM (IC50)


[In Vitro]

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].

[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.

[2]. Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H31Cl2N7O4

[ Molecular Weight ]:
624.52

Related Compounds