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。
| Cas No. | 1386979-55-0 |
| 别名 | Dyrk1B/A-IN-1 |
| Canonical SMILES | ClC1=CC=C(C(NCC2=CC(Cl)=CC=C2)=O)C=C1NC(C3=CC4=CN=C(OC)N=C4N=C3O)=O |
| 分子式 | C23H17Cl2N5O4 |
| 分子量 | 498.32 |
| 溶解度 | DMSO : 5 mg/mL (10.03 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
