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|606015-10MG||Glass bottle||10 mg||
|Overview||A cell-permeable, non-toxic pyridineisothiazolone compound that acts as a potent, reversible, and ATP-competitive inhibitor of human Thymidylate kinase (TMPK) (IC50 = 610 nM; Ki = 180 nM). Does not affect the activity of Thymidine kinase 1 (TK1) (IC50 > 10 µM). Its action appears to involve blocking the interaction of Mg2+ with Asp15 in the catalytic domain. Shown to specifically reduce dTTP (deoxythymidine triphosphate) by 30 to 40% in HCT-116 p53-/- cells, without affecting dATP, dCTP, and dGTP levels. Significantly increases (3 to 35 fold) the sensitivity of a variety of tumor cell lines to doxorubicin (Cat. No. 324380), and shrinks tumor size in HCT-116 p53-/- xenografted mouse model (doxorubicin, 1.25 mg/kg twice a week, i.p.; YMU1, 5 mg/kg thrice a week, i.p.).|
|Synonyms||Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate, TMPK Inhibitor|
|References||Hu, C.M., et al. 2012. Cancer Cell 22, 36.|
|Structure formula Image|
|Primary Target IC<sub>50</sub>||610 nM|
|Primary Target K<sub>i</sub>||180 nM for TMPK|
|Purity||≥99% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem SDS
|Hu, C.M., et al. 2012. Cancer Cell 22, 36.|
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