USP1-IN-9 

USP1-IN-9 (Compound 1m) is reversible and noncompetitive USP1 inhibitors with an IC₅₀ of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer^[1].

USP1-IN-9 (20, 100, 500 nM, 24 h) elevates the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner. USP1-IN-9 demonstrates an increase in Ub-PCNA even at concentrations as low as 20 nM in nonsmall cell lung cancer (NSCLC) cells^[1].
USP1-IN-9 (0.5 μM, 7 days) exhibites a substantial inhibition of the colony forming capacity of NSCLC cells^[1].
USP1-IN-9 (1 nM, 24 h) alone results in a minor cell cycle arrest in olaparib-resistant breast cancer cells, whereas the combination of olaparib (HY-10162) and USP1-IN-9 can induce cell cycle arrest^[1].
USP1-IN-9 (100 nM, 7 days) combined with olaparib can potentiate breast cancer cells to olaparib killing^[1].

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

USP1-IN-9 (10 mg/kg, i.g.) is absorbed rapidly and shows good metabolic stability on male ICR mice^[1].
合并列 符号