| Bioactivity | JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3 ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230))[1]. |
| Invitro | JCS-1 (0.1-10000 nM, 24 h) 以剂量依赖性方式降解 MOLM-14 细胞中的 DcpS，其DC50 为 87 nM[1]。JCS-1 (1 μM) 在 MOLM-14 细胞中对 DcpS 的降解迅速且持续，降解在处理后 2 小时内就迅速发生，最大降解发生在 12 到 24 h之间[1]。JCS-1 (1 μM, 每 3 天一次，共 12 天) 抑制 MOLM-14 细胞增殖和活力，IC50值为 1.1 μM[1]。JCS-1 (1 μM, 6 h) 影响 MOLM-14 细胞的 mRNA 库, 显著增加 SNORD99 和 DDX24 表达[1]。内切酶抑制剂 MLN4924 (HY-70062) 和蛋白酶体抑制剂 Epoxomicin (HY-13821) 可抑制 JCS-1 引起的降解[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JCS-1 相关抗体: |
| Formula | C62H79N9O12S |
| Molar Mass | 1174.41 |
| 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]. Swartzel, et al. Targeted Degradation of mRNA Decapping Enzyme DcpS by a VHL-Recruiting PROTAC. ACS chemical biology. 2022, 17(7), 1789–1798. |