85-2074-48　［取扱停止］Mirk/Dyrk1B Inhibitor, Compound A (N-(2-Chloro-5-(3-chlorobenzylcarbamoyl)phenyl)-2-methoxy-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, N-(2-Chloro-5-((3-chlorobenzyl)carbamoyl)phenyl)-7-hydroxy-2-methoxypyrido[2,3-d]pyrimidine-6-carboxamide) 10mg　217551

特徴

• A cell-permeable dihydropyridopyrimidine-carboxamide compound that acts as a potent and reversible inhibitor of Mirk/Dyrk1B and Dyrk1A kinases (IC50 = 68 and 22nM). Exhibits very high selectivity for Mirk/Dyrk1B compared to Abl, Flt3, and MARK1 (64, 56 and 73% inhibition at 10uM, respectively) and a panel of 46 other kinases. Shown to induce activation of caspase-3 and sensitize tumor cells to the action of gemcitabine and cisplatin, possibly by de-stabilizing p27. Preferentially increases cycling in Mirk-elevated quiescent pancreatic cancer cells (SU86.86, Panc1, AsPc1, and SW620 at ~1uM). Also, shown to increase level of superoxides in quiescent pancreatic tumor cells (Panc1, SU86.86, and AsPc1) by blocking SOD2 and SOD3 activities.
• Formula:C23H17Cl2N5O4
• Solubility:DMSO
• Molar Mass:498.3
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.