606015 Sigma-AldrichThymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem
The Thymidylate Kinase Inhibitor, YMU1 controls the biological activity of Thymidylate Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
More>> The Thymidylate Kinase Inhibitor, YMU1 controls the biological activity of Thymidylate Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: TMPK Inhibitor, Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
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Overview
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| Description | |
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| 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.). |
| Catalogue Number | 606015 |
| Brand Family | Calbiochem® |
| Synonyms | TMPK Inhibitor, Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate |
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| References | Hu, C.M., et al. 2012. Cancer Cell 22, 36. |
| Product Information | |
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| CAS number | 902589-96-2 |
| Form | White solid |
| Hill Formula | C₁₇H₂₂N₄O₄S |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
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| Biological Information | |
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| Primary Target | TMPK |
| Primary Target IC<sub>50</sub> | 610 nM |
| Primary Target K<sub>i</sub> | 180 nM for TMPK |
| Purity | ≥99% by HPLC |
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| Cell permeable | Y |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Catalogue Number | GTIN |
| 606015 | 0 |
Documentation
Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem SDS
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Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem Certificates of Analysis
| Title | Lot Number |
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| 606015 |
References
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| Hu, C.M., et al. 2012. Cancer Cell 22, 36. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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