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

Mirk-IN-1 (Dyrk1B/A-IN-1) 是一种有效的 Dyrk1B(Mirk kianse) 和 Dyrk1A 抑制剂,IC50 分别为 68±48 nM 和 22±8 nM。

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Mirk-IN-1 (Dyrk1B/A-IN-1)的二维码
  • 库存: 现货
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  • 10mg
    ¥1712.00
    1370.00
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  • 50mg
    ¥6850.00
    5480.00
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  • 货号: ajce49880
  • CAS: 1386979-55-0
  • 别名: Dyrk1B/A-IN-1
  • 分子式: C23H17Cl2N5O4
  • 分子量: 498.32
  • 纯度: >98%
  • 溶解度: DMSO : 5 mg/mL (10.03 mM);Water : < 0.1 mg/mL (insoluble)
  • 储存: Store at -20°C
  • 库存: 现货

Background

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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