531131 USP1-UAF1 Inhibitor, ML323 - Calbiochem

531131
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₄N₆

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31131.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, non-toxic triazolylbenzyl-pyrimidinamine compound that acts as a highly selective, potent, and reversible inhibitor of ubiquitin-specific protease 1 (USP1)-USP1 associated factor 1 (UAF1) deubiquitinase (DUB) (IC50 = 76, 174, and 820 nM in Ub-Rhodamine; K63 linked diubiquitin; and Ub-PCNA substrate based assays) without disrupting USP1-UAF1 association. The inhibition appears to be allosteric in nature with inhibition constants of 68 nM and 183 nM (for free enzyme and enzyme-substrate complex, respectively). Displays excellent selectivity over 18-DUBs including USP1 and USP46-UAF1, related deSUMOylases & deneddylases, 70 unrelated proteases, and 451 kinases. Effectively sensitizes cisplatin-resistant NSCLC H596 cells and U2OS osteosarcoma cells to cisplatin (Cat. No. 232120) and blocks cell cycle at the S phase (EC50 = 171 and 59 nM for 1:1 and 1:4 ratio of cisplatin to ML323 in H596 cells).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531131
          Brand Family Calbiochem®
          SynonymsN-(4-(1H-1,2,3-Triazol-1-yl)benzyl)-2-(2-isopropylphenyl)-5-methylpyrimidin-4-amine, USP1–UAF1 Deubiquitinase complex Inhibitor, ML 323
          References
          ReferencesDexheimer, T.S., et al. 2014. J. Med. Chem. 57, in press.
          Liang, Q., et al. 2014. Nat Chem Biol. 10, 298.
          Product Information
          FormOff-white powder
          Hill FormulaC₂₃H₂₄N₆
          Chemical formulaC₂₃H₂₄N₆
          ReversibleY
          Applications
          Biological Information
          Primary TargetUSP1-UAF1 deubiquitinase (DUBs) complex
          Purity≥98% 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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          USP1-UAF1 Inhibitor, ML323 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Dexheimer, T.S., et al. 2014. J. Med. Chem. 57, in press.
          Liang, Q., et al. 2014. Nat Chem Biol. 10, 298.
          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.

          Revision31-July-2014 JSW
          SynonymsN-(4-(1H-1,2,3-Triazol-1-yl)benzyl)-2-(2-isopropylphenyl)-5-methylpyrimidin-4-amine, USP1–UAF1 Deubiquitinase complex Inhibitor, ML 323
          DescriptionA cell-permeable, non-toxic triazolylbenzyl-pyrimidinamine compound that acts as a highly selective, potent, and reversible inhibitor of ubiquitin-specific protease 1 (USP1)-USP1 associated factor 1 (UAF1) deubiquitinase (DUB) (IC50 = 76, 174, and 820 nM in Ub-Rhodamine; K63 linked diubiquitin; and Ub-PCNA substrate based assays) without disrupting USP1-UAF1 association. The inhibition appears to be allosteric in nature with inhibition constants of 68 nM and 183 nM (for free enzyme and enzyme-substrate complex, respectively). Displays excellent selectivity over 18-DUBs including USP1 and USP46-UAF1, related deSUMOylases & deneddylases, 70 unrelated proteases, and 451 kinases. Effectively sensitizes cisplatin-resistant NSCLC H596 cells and U2OS osteosarcoma cells to cisplatin (Cat. No. 232120) and blocks cell cycle at the S phase (EC50 = 171 and 59 nM for 1:1 and 1:4 ratio of cisplatin to ML323 in H596 cells).
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₂₄N₆
          Purity≥98% by HPLC
          SolubilityDMSO (100 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesDexheimer, T.S., et al. 2014. J. Med. Chem. 57, in press.
          Liang, Q., et al. 2014. Nat Chem Biol. 10, 298.