| Bioactivity | AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA[1]. |
| Invitro | AurkA allosteric-IN-1 (100 μM; 48 h) 在不同细胞类型间 (包括肺癌细胞系和直肠癌细胞系) 差异诱导了对细胞周期的阻滞作用[1]。AurkA allosteric-IN-1 (20 μM; 48 h) 可下调癌细胞中磷酸组蛋白 H3 的水平[1]。AurkA allosteric-IN-1 (25-400 μM; 48 h) 对 HeLa 细胞表现出显著抗细胞增殖活性，并与 PHA-767491 (HY-13461) 具有协同作用，使其抗增殖活性被进一步放大[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> AurkA allosteric-IN-1 相关抗体: Cell Cycle Analysis[1] Cell Line: |
| Formula | C20H16N2O3 |
| Molar Mass | 332.35 |
| 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]. Lee H, et al. Discovery of N-benzylbenzamide-based allosteric inhibitors of Aurora kinase A. Bioorg Med Chem. 2024 Mar 15;102:117658. |