2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. USP1-IN-17

USP1-IN-17 是一种具有口服活性的 USP1/UAF1 复合物抑制剂。USP1-IN-17 可强效抑制携带 BRCA1 突变的人乳腺癌细胞 MDA-MB-436 的增殖，其 IC50 为 8.1 nM。USP1-IN-17 结合 USP1 稳定酶构象，削弱去泛素化功能，提高 PCNA 单泛素化水平，并抑制癌细胞增殖，且会诱导 DNA 损伤积累。USP1-IN-17 可用于 BRCA1 突变癌症的研究。

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USP1-IN-17

USP1-IN-17 Chemical Structure

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USP1-IN-17 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

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USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

USP1-IN-17 (compound 18) (25-100 nM) 可强效抑制 USP1/UAF1 复合物，其 IC50 值 ＜ 50 nM，在 25 nM 至 100 nM 的浓度范围内抑制率可达 45.5% 至 76.0%[1]。
USP1-IN-17 (6 days) 能抑制 BRCA1 突变型 MDA-MB-436 乳腺癌细胞的增殖，IC50 为 8.1 nM，且具有高选择性，在 BRCA1 野生型 MCF-7 和 BT549 细胞中 IC50 值超过 10 μM，选择性比率超过 1200 倍[1]。
USP1-IN-17 (25-100 nM, 48 h) 以剂量依赖方式增加 BRCA1 突变型人乳腺癌细胞 MDA-MB-436 中 PCNA 单泛素化水平和 γH2AX 水平，表明其可诱导 DNA 损伤和复制应激[1]。

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

USP1-IN-17 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-436 human breast cancer cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
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.
药代动力学
(Parmacokinetics)
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
分子量

564.52

Formula

C26H23F3N10O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

USP1-IN-17 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

USP1-IN-17DeubiquitinaseDUBsBRCA1-wild-type cellsDNA damageMDA-MB-436 human breast cancer cellsUSP1BRCA1-mutant cellsdeubiquitinationBRCA1-mutant cancerscancer cell proliferationPCNA monoubiquitinationUSP1/UAF1 complexInhibitorinhibitorinhibit

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