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

606015
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      Overview

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      606015-10MG
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          Glass bottle 10 mg
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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
          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.