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Chemical Structure : I-138
CAS No.: 2098211-50-6
Catalog No.: PC-49689Not For Human Use, Lab Use Only.
I-138 (I 138) is a potent, specific small molecule USP1-UAF1 inhibitor with IC50 of 4.1 nM, binds to USP1-UAF1 at an allosteric pocket synergistically with ubiquitin.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $388 | In stock | |
| 10 mg | $588 | In stock | |
| 25 mg | $898 | In stock | |
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| 100 mg | Get quote |
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I-138 (I 138) is a potent, specific small molecule USP1-UAF1 inhibitor with IC50 of 4.1 nM, binds to USP1-UAF1 at an allosteric pocket synergistically with ubiquitin.
I-138 displays exquisite selectivity (>2,000-fold) across a panel of 45 deubiquitinating enzymes (Ubiquigent DUBprofiler) at 10 uM, including the closely related USP12-UAF1 and USP46-UAF1 complexes.
I-138 treatment (500 nM, 4 hours) increased PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT but not knockout cells, induced the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, also ablated USP1 autocleavage in cells.
I-138 (0-10 uM) selectively caused loss of viability (IC50=50 nM) and replication stress in BRCA1/2 mutant cells (MDA-MB-436 cell), but not the WT breast cancer cell line HCC1954.
I-138 displayed improved potency and physiochemical properties suitable for in vivo studies compared with ML323.
I-138 demonstarted strongly synergistic effect with PARP inhibitor Olaparib in a BRCA1/2-dependent manner in vitro, and in mice bearing MDA-MB-436 tumors.
| M.Wt | 492.51 | |
| Formula | C26H23F3N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(2-isopropylphenyl)-9-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-7,9-dihydro-8H-purin-8-one |
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1. Patent WO/2017/087837.
2. Antoine Simoneau, et al. Mol Cancer Ther. 2023 Feb 1;22(2):215-226.
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