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606015 Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem

606015
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606015-10MG
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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
      Applications
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Thymidylate Kinase Inhibitor, YMU1 - CAS 902589-96-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      606015

      References

      Reference overview
      Hu, C.M., et al. 2012. Cancer Cell 22, 36.
      Data Sheet

      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.

      Revision11-October-2013 JSW
      SynonymsTMPK Inhibitor, Ethyl 4-(2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl)piperazine-1-carboxylate
      DescriptionA 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.).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number902589-96-2
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (3.3 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesHu, C.M., et al. 2012. Cancer Cell 22, 36.