USP1-IN-17 

USP1-IN-17 is an orally active USP1/UAF1 complex inhibitor. USP1-IN-17 exhibits potent anti-proliferative activity against BRCA1-mutant human breast cancer MDA-MB-436 cells, with an IC₅₀ value of 8.1 nM. USP1-IN-17 binds to USP1 to stabilize the enzyme conformation, impairs deubiquitination function, elevates the monoubiquitination level of PCNA, inhibits cancer cell proliferation, and induces DNA damage accumulation. USP1-IN-17 can be used for the research of BRCA1-mutated cancers^[1].

USP1-IN-17 (compound 18) (25-100 nM) potently inhibits the USP1/UAF1 complex with an IC₅₀ of < 50 nM, achieving 45.5% to 76.0% inhibition at concentrations ranging from 25 nM to 100 nM^[1].
USP1-IN-17 (6 days) can suppress the proliferation of BRCA1-mutant MDA-MB-436 breast cancer cells with an IC₅₀ of 8.1 nM and shows high selectivity, with IC₅₀ values over 10 μM in BRCA1 wild-type MCF-7 and BT549 cells, achieving a selectivity ratio exceeding 1200-fold^[1].
USP1-IN-17 (25-100 nM, 48 h) dose-dependently increases PCNA monoubiquitination and γH2AX levels in BRCA1-mutant MDA-MB-436 human breast cancer cells, indicating induction of DNA damage and replication stress^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

564.52

C₂₆H₂₃F₃N₁₀O₂

COC1=C(C2=NC(NN=C3C(N)=O)=C3C(NCC4=CC=C(C5=NC(C(F)(F)F)=CN5C)C=C4)=N2)C(C6CC6)=NC=N1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhao T, et al. Discovery and optimization of 1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide derivatives as USP1 inhibitors for BRCA1-mutant cancer treatment. Bioorg Chem. 2026;175:109820.