531131 USP1-UAF1 Inhibitor, ML323 - Calbiochem

531131
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₂₄N₆

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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
      Quality LevelMQ100
      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.