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Description: Potent and selective USP1-UAF1 allosteric inhibitor
Chemical Name: 5-Methyl-2-[2-(1-methylethyl)phenyl]-N-[[4-(1H-1,2,3-triazol-1-yl)phenyl]methyl]-4-pyrimidinamine
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective allosteric inhibitor of USP1-UAF1 deubiquitinase complex (IC50 = 76 nM). Exhibits selectivity for USP1-UAF1 over a panel of enzymes, including other deuquitinating enzymes. Inhibits deubiquitination of PCNA and FANCD2 and sensitizes cisplatin-resistant H596 cells to cell death induced by cisplatin (Cat. No. 2251) in vitro.
Technical Data
| M. Wt | 384.48 |
| Formula | C23H24N6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1572414-83-5 |
| PubChem ID | 60167849 |
| InChI Key | VUIRVWPJNKZOSS-UHFFFAOYSA-N |
| Smiles | CC(C)C1=C(C=CC=C1)C1=NC=C(C)C(NCC2=CC=C(C=C2)N2C=CN=N2)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.45 | 100 | |
| ethanol | 38.45 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 384.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.6 mL | 13 mL | 26.01 mL |
| 5 mM | 0.52 mL | 2.6 mL | 5.2 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Liang et al (2014) A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses. Nat.Chem.Biol. 10 298 PMID: 24531842
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Keywords: ML 323, ML 323 supplier, ML323, DUB, inhibitors, inhibits, deubiquitinase, USP1, UAF1, potent, selective, Deubiquitinating, Enzymes, 6435, Tocris Bioscience
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