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606015 Thymidylate 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.

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

606015
  
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Description
OverviewA 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 Number606015
Brand Family Calbiochem®
SynonymsTMPK Inhibitor, Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
References
ReferencesHu, C.M., et al. 2012. Cancer Cell 22, 36.
Product Information
CAS number902589-96-2
FormWhite solid
Hill FormulaC₁₇H₂₂N₄O₄S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetTMPK
Primary Target IC<sub>50</sub>610 nM
Primary Target K<sub>i</sub>180 nM for TMPK
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Use only fresh DMSO for reconstitution.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Katalogové číslo GTIN
606015 0