| Bioactivity | USP1-IN-9 (Compound 1m) is reversible and noncompetitive 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]. |
| Invitro | 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. 0 --> USP1-IN-9 相关抗体: Western Blot Analysis[1] Cell Line: |
| 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 |
| CAS | 2925548-22-5 |
| Formula | C29H26F3N7O2 |
| Molar Mass | 561.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. [1] Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors[j]. Eur J Med Chem. 2024 Jun 14;275:116568.https://pubmed.ncbi.nlm.nih.gov/38889606/ [2]. Li H, et al. Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors[J]. Eur J Med Chem. 2024 Jun 14;275:116568. |
USP1-IN-9
CAS: 2925548-22-5 F: C29H26F3N7O2 W: 561.56
USP1-IN-9 (Compound 1m) is reversible and noncompetitive USP1 inhibitors with an IC50 of 8.8 nM, which is designed and s
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