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.
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- 分子式: C26H23F3N10O2
- 分子量:564.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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Cell Line:MDA-MB-436 human breast cancer cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Increased PCNA monoubiquitination and γH2AX levels in BRCA1-mutant MDA-MB-436 human breast cancer cells, indicating induction of DNA damage and replication stress.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | MRT |
|---|---|---|---|---|---|---|---|
| Rat[1] | 3 mg/kg | p.o. | 3.0 h | 0.3 h | 7.0 ng/mL | 23.5 ng·h/mL | 3.62 h |
化学情報
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分子量 564.52
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分子式 C26H23F3N10O2
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SMILES
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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
USP1-IN-17 関連分類
HY-183363 関連分類
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