USP1 inhibitor 38-P2

Chemical Structure : USP1 inhibitor 38-P2

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货号: PC-24052Not For Human Use, Lab Use Only.

USP1 inhibitor 38-P2 is a potent, selective, reversible, and noncompetitive ubiquitin-specific protease 1 (USP1) inhibitor with IC50 of 3.8 nM (USP1-UAF1).

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

USP1 inhibitor 38-P2 is a potent, selective, reversible, and noncompetitive ubiquitin-specific protease 1 (USP1) inhibitor with IC50 of 3.8 nM (USP1-UAF1).
38-P2 exhibits potent antiproliferative activity against NCI-H1299 cells with IC50 of 0.5 nM.
38-P2 strongly inhibits the proliferation of BRCA1-deficient MDA-MB-436 cells with an IC50 value of <0.03 nM, with no activity in normal cell lines HL-7702 and IM-9 (IC50s > 10 μM).
38-P2 selectively inhibits the cleavage of K63-linked diubiquitin by USP1-UAF1, while exhibiting negligible inhibition of other tested USPs, including USP4, USP7, USP8, USP9X, USP15, and USP25.
38-P2 induces S-phase arrest in BRCA1-deficient MDA-MB-436 cells and G2/M phase arrest in MDA-MB-436/OP cells, enhances the sensitivity of resistant cells to Olaparib.
38-P2 (75 mg/kg and 150 mg/kg daily, oral) significantly inhibited the growth of MDA-MB-436 xenografts on MDA-MB-436 xenografts in nude mice, demonstrated an increase in Ub-PCNA protein levels.

物理化学性质&存储条件

分子量	605.62
分子式	C31H30F3N7O3
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	(R)-2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-4-(3-(4-(1-isopropyl-4-(trifluoromethyl)-1H-imidazol-2-yl)phenyl)morpholino)furo[3,2-d]pyrimidine

参考文献

1. Zhang J, et al. J Med Chem. 2025 Feb 4. doi: 10.1021/acs.jmedchem.4c02792.