2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. USP1-IN-15

USP1-IN-15 是一种口服有效且具有选择性的 USP1 抑制剂，其 IC50 为 12.3 nM。USP1-IN-15 对 USP1 具有高度特异性，对所有脱靶去泛素化酶的抑制作用可忽略不计。 USP1-IN-15 可抑制细胞集落形成诱导 S 期阻滞，并稳定泛素化 PCNA。USP1-IN-15 还显示出协同抗增殖活性，并在体内实现了显著的肿瘤生长抑制。USP1-IN-15 可用于 BRCA 突变型乳腺癌的研究。

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USP1-IN-15

USP1-IN-15 Chemical Structure

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USP1-IN-15 相关抗体

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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-15 is an orally active and selective USP1 inhibitor with an IC50 of 12.3 nM. USP1-IN-15 has a high specificity for USP1 with negligible inhibition against all off-target DUBs. USP1-IN-15 suppresses colony formation, induces S-phase arrest, and stabilizes ubiquitinated PCNA. USP1-IN-15 also shows synergistic antiproliferative activity. USP1-IN-15 achieves significant tumor growth inhibition in vivo. USP1-IN-15 can be used for BRCA-mutated breast cancer[1].

IC50 & Target[1]

USP1

12.3 nM (IC50)

体外研究
(In Vitro)

USP1-IN-15 (compound 43) (14 天) 平衡了强效抗增殖活性与良好代谢稳定性的特性：其在 MDA-MB-436 细胞中的 IC50 为 0.07 μM，且代谢稳定性半衰期 (t1/2) 超过 120 分钟[1]。
USP1-IN-15 (1 μM) 对 USP1 具有高度特异性，对所有脱靶去泛素化酶 (包括 USP5、USP7、USP8、USP9X、USP14、USP15、USP25、USP28、BAP1 和 OTUD1) 的抑制作用可忽略不计[1]。
USP1-IN-15 (0-1000 nM, 0-168 小时) 在 MDA-MB-436 乳腺癌细胞中，能剂量和时间依赖性地强效、持久地抑制增殖细胞核抗原 (PCNA) 的去泛素化并且诱导了 p-H2AX 蛋白[1]。
USP1-IN-15 (100-1000 nM, 48 小时 或 2-3 周) 在 MDA-MB-436 乳腺癌细胞中诱导了 S 期阻滞[1]。
USP1-IN-15 (0.1-10 μM, 7 天或 2-3 周) 在 MDA-MB-436 细胞中与 Olaparib (HY-10162) 联用时，相比单药治疗，能剂量依赖性地增强生长抑制效果[1]。
USP1-IN-15 (1 μM, 48 h) 在 MDA-MB-436 细胞中通过与 Olaparib 联用通过增强诱导 DNA 损伤和细胞周期阻滞，表现出卓越的协同活性[1]。

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

USP1-IN-15 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 0, 6, 24, 48, 72, 96, 120, 144, and 168 h
Result: Exhibited deubiquitination inhibition, increased the protein level of ubiquitinated PCNA (ubPCNA) and induced the protein level of p-H2AX0 at 48 h and beyond in range of 0-168 h and 300 nM.
Increased the protein level of ubPCNA in a dose-dependent manner at lower concentrations (100 and 300 nM) .
Showed significantly higher ubPCNA levels at 100, 300, and 1000 nM.
Elevated p-H2AX protein levels at 100, 300, and 1000 nM.

Immunofluorescence[1]

Cell Line: MDA-MB-436 cells
Concentration: 300 nM
Incubation Time: 72 h
Result: Induced the superior p-H2AX signal intensity and more nuclear foci.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-436 cells
Concentration: 100, 300, 1000 nM
Incubation Time: 2-3 weeks
Result: Inhibit the growth of clones in a dose-dependent manner.
Demonstrated superior antiproliferative activity, reducing colony counts by 55.99 % (300 nM) and 66.89% (1000 nM) .

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 100, 300, 1000 nM
Incubation Time: 48 h
Result: Induced S-phase arrest at a concentration range of 100-1000 nM.

Cell Viability Assay[1]

Cell Line: MDA-MB-436 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 7 days
Result: Revealed stronger cell growth inhibition in combination regimens when combination with Olaparib.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced significant cell cycle arrest with marked accumulation of cells in the S phase but induced significant accumulation of MDA-MB-436 cells at S and G2/M phases when combined with Olaparib.
Exhibited pronounced synergistic effects, resulting in a more robust cell cycle perturbation when combined with Olaparib.

Western Blot Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Elevated p-H2AX levels with or without combination with Olaparib but had a better effect when combinated with Olaparib.
体内研究
(In Vivo)

USP1-IN-15 (compound 43) (40 mg/kg，口服，每日一次，持续 45 天) 在在异种移植瘤小鼠模型中表现出显著的单一药剂抗肿瘤活性，与 Olaparib 联用产生协同增强效应，并显示出极低的全身毒性[1]。

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

Animal Model: MDA-MB-436 cells (5 × 106) induced-female nude mice(6-9 weeks, 17-19 g)[1]
Dosage: 40 mg/kg
Administration: p.o., once daily, for 45 days, with or without combination with Olaparib (30 mg/kg)
Result: Exhibited the most potent antitumor activity.
Exhibiting the most significant reduction (TGI = 82.734%) in tumor weight.
Observed no significant differences in body weight.
Demonstrated no statistically significant differences in organ indices of heart, liver, lung, and kidney.
Resulted significant reductions in Ki67-positive cells in both monotherapy or combination groups.
Elevated levels of ubPCNA in monotherapy.
Exhibited the highest level of p-H2AX, consistent with its robust DNA damage-inducing capability.
分子量

599.57

Formula

C30H24F3N9O2
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-15 相关分类

  • 摩尔计算器

  • 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-15DeubiquitinaseDUBsUSP1S-phase arrestubiquitinated PCNABRCA-mutated breast cancerInhibitorinhibitorinhibit

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