Mirk-IN-1 (Dyrk1B/A-IN-1) (Synonyms: Dyrk1B/A-IN-1) |
| رقم الكتالوجGC32819 |
Mirk-IN-1 (Dyrk1B / A-IN-1) هو مثبط قوي لـ Dyrk1B (Mirk kianse) و Dyrk1A مع IC50 لـ 68± ؛ 48 نانومتر و 22± ؛ 8 نانومتر على التوالي.
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Cas No.: 1386979-55-0
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
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