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Mirk-IN-1

Chemical Structure : Mirk-IN-1

CAS No.: 1386979-55-0

Mirk-IN-1 (Dyrk1B/A-IN-1)

Catalog No.: PC-43249Not For Human Use, Lab Use Only.

Mirk-IN-1 is a potent, specific inhibitor of Dyrk1B (Mirk kianse) and Dyrk1A with IC50 of 68 nM and 22 nM respectively, shows SW620 cell IC50 of 1.9 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Mirk-IN-1 is a potent, specific inhibitor of Dyrk1B (Mirk kianse) and Dyrk1A with IC50 of 68 nM and 22 nM respectively, shows SW620 cell IC50 of 1.9 uM; weakly inhibits DYRK1A, ABL, FLT3, and MARK1 with 88%, 64%, 56% and 73% at 10 uM, shows no activity against the other kinases in the Caliper assay panel; blocks tumor cells from undergoing reversible arrest in a quiescent G(0) state and enables some cells to exit quiescence, elevates ROS levels and DNA damage detected by increased phosphorylation of the histone protein H2AX and by S-phase checkpoints; sensitizes cells to gemcitabine and cisplatin.

Physicochemical Properties

M.Wt 498.3182
Formula C23H17Cl2N5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Pyrido[2,3-d]pyrimidine-6-carboxamide, N-[2-chloro-5-[[[(3-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxo-

References

1. Ewton DZ, et al. Mol Cancer Ther. 2011 Nov;10(11):2104-14.

2. Anderson K, et al. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5.

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