Cas No.: | 1386979-55-0 |
Chemical Name: | Mirk-IN-1 |
Synonyms: | TC-S 7004;A-IN-1;Dyrk1B;Mirk-IN-1;Dyrk1B/1A-IN-9;Dyrk1B/A-IN-1;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-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxopyrido[2,3-d]pyrimidine-6-carboxamide;BDBM50444379;A908185;2-methoxy-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid [2-chloro-;Mirk inhibitor 1;Pyrido[2,3-d]pyrimidine-6-carboxamide, N-[2-chloro-5-[[[(3-chlorophenyl)methyl]amino]carbonyl]phenyl]-7,8-dihydro-2-methoxy-7-oxo- |
SMILES: | ClC1C([H])=C([H])C(C(N([H])C([H])([H])C2C([H])=C([H])C([H])=C(C=2[H])Cl)=O)=C([H])C=1N([H])C(C1C(N([H])C2C(=C([H])N=C(N=2)OC([H])([H])[H])C=1[H])=O)=O |
Formula: | C23H17Cl2N5O4 |
M.Wt: | 498.3182 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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; 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; 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; sensitizes cells to gemcitabine and cisplatin. |