531131 Sigma-AldrichUSP1-UAF1 Inhibitor, ML323 - CAS 1572414-83-5 - Calbiochem
A cell-permeable, selective, potent, and reversible inhibitor of USP1-UAF1 deubiquitinase (IC₅₀ = 76 nM in Ub-Rhodamine based assays). Does not disrupt USP1-UAF1 association.
More>> A cell-permeable, selective, potent, and reversible inhibitor of USP1-UAF1 deubiquitinase (IC₅₀ = 76 nM in Ub-Rhodamine based assays). Does not disrupt USP1-UAF1 association. Less<<同義語: N-(4-(1H-1,2,3-Triazol-1-yl)benzyl)-2-(2-isopropylphenyl)-5-methylpyrimidin-4-amine, USP1–UAF1 Deubiquitinase complex Inhibitor, ML 323
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概要
Replacement Information |
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主要スペック表
CAS # | Empirical Formula |
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1572414-83-5 | C₂₃H₂₄N₆ |
価格&在庫状況
カタログ番号 | 在庫状況 | 包装 | Qty/Pk | 価格 | 数量 | |
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5.31131.0001 |
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ガラスビン | 10 mg |
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Description | |
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Overview | A 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 Number | 531131 |
Brand Family | Calbiochem® |
Synonyms | N-(4-(1H-1,2,3-Triazol-1-yl)benzyl)-2-(2-isopropylphenyl)-5-methylpyrimidin-4-amine, USP1–UAF1 Deubiquitinase complex Inhibitor, ML 323 |
References | |
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References | Dexheimer, T.S., et al. 2014. J. Med. Chem. 57, in press. Liang, Q., et al. 2014. Nat Chem Biol. 10, 298. |
Product Information | |
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CAS number | 1572414-83-5 |
Form | Off-white powder |
Hill Formula | C₂₃H₂₄N₆ |
Chemical formula | C₂₃H₂₄N₆ |
Reversible | Y |
Quality Level | MQ100 |
Applications |
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Biological Information | |
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Primary Target | USP1-UAF1 deubiquitinase (DUBs) complex |
Purity | ≥98% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
Dimensions |
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Materials Information |
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Safety Information according to GHS |
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Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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カタログ番号 | GTIN |
5.31131.0001 | 04055977242638 |
Documentation
USP1-UAF1 Inhibitor, ML323 - CAS 1572414-83-5 - Calbiochem (M)SDS
タイトル |
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参考資料
参考資料の概要 |
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Dexheimer, T.S., et al. 2014. J. Med. Chem. 57, in press. Liang, Q., et al. 2014. Nat Chem Biol. 10, 298. |
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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.
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