1386979-55-0

1386979-55-0 structure

Name: TC-S 7004
Chemical Name: Mirk-IN-1
CAS Number: 1386979-55-0
Molecular Formula: C₂₃H₁₇Cl₂N₅O₄
Molecular Weight: 498.318
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK DYRK
Create Date: 2018-03-06 06:27:40
Modify Date: 2024-01-04 05:03:32
Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.IC50 value: 68±48/22±8 nM (Dyrk1B/Dyrk1A) [1]Target: Dyrk inhibitorMirk-IN-1 had an EC50 of 1.9 ±0.2 mmol/L on SW620 cells. At a much higher concentration of 10 mmol/L in a kinase assay, Mirk-IN-1 inhibited the activities of DYRK1A, ABL, FLT3, and MARK1 by88%, 64%, 56%, and 73%, respectively [1]. Mirk-IN-1 was able to block tumor cells from undergoing reversible arrest in a quiescent G0 state and enable some cells to exit quiescence [2].

Name	Mirk-IN-1
Synonyms	N-{2-Chloro-5-[(3-chlorobenzyl)carbamoyl]phenyl}-2-methoxy-7-oxo-1,7-dihydropyrido[2,3-d]pyrimidine-6-carboxamide Pyrido[2,3-d]pyrimidine-6-carboxamide, N-[2-chloro-5-[[[(3-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxo-

Description	Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.IC50 value: 68±48/22±8 nM (Dyrk1B/Dyrk1A) [1]Target: Dyrk inhibitorMirk-IN-1 had an EC50 of 1.9 ±0.2 mmol/L on SW620 cells. At a much higher concentration of 10 mmol/L in a kinase assay, Mirk-IN-1 inhibited the activities of DYRK1A, ABL, FLT3, and MARK1 by88%, 64%, 56%, and 73%, respectively [1]. Mirk-IN-1 was able to block tumor cells from undergoing reversible arrest in a quiescent G0 state and enable some cells to exit quiescence [2].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK Research Areas >> Cancer
References	[1]. Ewton DZ, et al. Inactivation of mirk/dyrk1b kinase targets quiescent pancreatic cancer cells. Mol Cancer Ther. 2011 Nov;10(11):2104-14. [2]. 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.