USP1-IN-9
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (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.
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- CAS 番号: 2925548-22-5
- 分子式: C29H26F3N7O2
- 分子量:561.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
[1]|
USP-1 8.8 nM (IC50) |
体外実験
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.
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Cell Line:NSCLC cells
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Concentration:20, 100, 500 nM
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Incubation Time:24 h
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Result:Elevated the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner in NSCLC cells.
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Cell Line:NSCLC cells
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Concentration:0.5 nM
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Incubation Time:7 days
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Result:Exhibited a substantial inhibition of the colony forming capacity of breast cancer cells compared to the untreated control.
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Cell Line:Breast cancer cells and olaparib-resistant breast cancer cells
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Concentration:1 nM
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Incubation Time:24 h
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Result:Resulted in a minor increase in cells within the S phase, whereas the combination of olaparib and USP1-IN-9 led to an accumulation of cells within the S phase and G2/M phase.
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Cell Line:Olaparib-resistant breast cancer cells
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Concentration:100 nM
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Incubation Time:7 days
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Result:Alone exhibited a reduction of 30% and did not demonstrate significant cell killing. The inhibition rate of colony formation was further elevated to 50 % combined with USP1-IN-9 and olaparib(100 nM).