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首页-小分子抑制剂&激动剂-Tyrosine Kinase-DYRK-Mirk-IN-1
Mirk-IN-1

Chemical Structure : Mirk-IN-1

CAS No.: 1386979-55-0

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

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
Mirk-IN-1 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.
Mirk-IN-1 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.
Mirk-IN-1 sensitizes cells to gemcitabine and cisplatin.

物理化学性质&存储条件

分子量 498.3182
分子式 C23H17Cl2N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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-

参考文献

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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