I-138 | UPS1 inhibitor | Probechem Biochemicals

Chemical Structure : I-138

CAS No.: 2098211-50-6

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I-138 (USP1 inhibitor I-138)

货号: 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.

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10 mg	￥3980	In stock
25 mg	￥5880	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	492.51
分子式	C26H23F3N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-isopropylphenyl)-9-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-7,9-dihydro-8H-purin-8-one

参考文献

1. Patent WO/2017/087837.

2. Antoine Simoneau, et al. Mol Cancer Ther. 2023 Feb 1;22(2):215-226.

I-138 (USP1 inhibitor I-138)

生物&药学活性

物理化学性质&存储条件

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I-138 (USP1 inhibitor I-138)

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物理化学性质&存储条件

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