2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. USP1-IN-9

USP1-IN-9 (Compound 1m) 是可逆的且非竞争性的泛素化特异性酶 (USP1) 抑制剂， IC50 值为 8.8 nM。它是在 ML323(HY-17543) 和 KSQ-4279(HY-145471) 结构的基础上被设计合成为吡啶[2,3-d]嘧啶-7(8H)- 1衍生物。USP1-IN-9 对 USP1/UAF 有很好的抑制作用，并且对乳腺癌细胞有很强的抗增殖作用。USP1-IN-9 与 PARP 抑制剂奥拉帕利布(HY-10162) 联合使用可增强对的 MDA-MB-436/OP 细胞的杀伤作用。USP1-IN-9 有望用于癌症领域的研究。

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USP1-IN-9 Chemical Structure

USP1-IN-9 Chemical Structure

CAS No. : 2925548-22-5

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USP1-IN-9 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

查看所有亚型
USP1 USP2 USP7 USP8 USP30 UCHL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

：结束 是行
USP1-IN-9在小鼠体内的药动学参数[1]

药代动力学分析[1]
生物活性

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[1].
IC50 & Target[1]

USP-1

8.8 nM (IC50)

体外研究
(In Vitro)

USP1-IN-9 (20, 100, 500 nM, 24 h) 在非小细胞肺癌细胞 (NSCLC) 中以剂量依赖性的方式升高了单泛素化增殖细胞核抗原 (Ub-PCNA) 的水平，且 USP1-IN-9 在低至 20 nM 的浓度下也显示出Ub-增殖细胞核抗原的增加[1]。
USP1-IN-9 (0.5 μM, 7 days) 对 NSCLC 细胞的集落形成能力有显著的抑制作用[1]。
USP1-IN-9 (1 nM, 24 h) 在奥拉帕利布耐药的乳腺癌细胞中单独处理细胞周期轻微阻滞，而奥拉帕利布 (HY-10162) 和 USP1-IN-9 联合作用可引起细胞周期阻滞[1]。
USP1-IN-9 (100 nM, 7 days) 和奥拉帕利布联合使用能增强奥拉帕利布对乳腺癌细胞的杀伤作用[1]。

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

USP1-IN-9 相关抗体:

Western Blot Analysis[1]

Cell Line: NSCLC cells
Concentration: 20, 100, 500 nM
Incubation Time: 24 h
Result: Elevated the monoubiquitinated PCNA (Ub-PCNA) levels in a dose-dependent manner in NSCLC cells.

Cell Viability Assay[1]

Cell Line: NSCLC cells
Concentration: 0.5 nM
Incubation Time: 7 days
Result: Exhibited a substantial inhibition of the colony forming capacity of breast cancer cells compared to the untreated control.

Cell Cycle Analysis[1]

Cell Line: Breast cancer cells and olaparib-resistant breast cancer cells
Concentration: 1 nM
Incubation Time: 24 h
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.

Cell Viability Assay[1]

Cell Line: Olaparib-resistant breast cancer cells
Concentration: 100 nM
Incubation Time: 7 days
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).
体内研究
(In Vivo)

USP1-IN-9 (10 mg/kg, i.g.) 在雄性ICR小鼠中被迅速吸收，并表现出良好的代谢稳定性[1]。
合并列 符号

： 代表后面的三列被合并 是列
Parameters Dose (mg/kg,po) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) T1/2 (h)
USP1-IN-9 10 0.25 4780 ± 2090 35,800 ± 13,500 7.61 ± 4.67

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

Animal Model: male ICR mice
Dosage: 10 mg/kg
Administration: i.g., a single dose
Result: Was absorbed rapidly and showed good metabolic stability with a long half-life of 7.61 h on male ICR mice.
分子量

561.56

Formula

C29H26F3N7O2

CAS 号 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-9 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-92925548-22-5DeubiquitinaseDUBsantiproliferation effectolaparib-resistant breast cancer cellsmale ICR miceInhibitorinhibitorinhibit

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