| Bioactivity | YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner[1]. |
| Invitro | YL5084 (0.001-100 μM; 72 小时) 在 MM.1S 细胞中表现出剂量依赖性抗增殖作用，GR50 值为 200-300 nM[1]。 YL5084 (0.5, 2.5 μM; 24 小时) 诱导细胞凋亡[1]。 YL5084 对 PIKFYVE (KdELECT 结合测定中的 KD=5000 nM) 表现出较弱的抑制作用[1]。 YL5084 在人和小鼠微粒体中具有中等代谢稳定性，半衰期分别为 16 分钟和 11 分钟[1]。 Cell Proliferation Assay[1] Cell Line: |
| Name | YL5084 |
| CAS | 2440199-73-3 |
| Formula | C35H36N8O2 |
| Molar Mass | 600.71 |
| 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]. Wenchao Lu, et al. Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1. J Med Chem. 2023 Mar 9;66(5):3356-3371. |