- 产品描述:
ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50 values of 32 μM and >100 μM, respectively)
- 靶点: IC50: 3 nM (SAE/SUMO1), 11 nM (SAE/SUMO2);E1/E2/E3Enzyme
- 体外研究:
ML-792 (0.0007-5 μM; 4 hours) inhibits SAE and SUMO-pathway activities in HCT116 cells. ML-792 (0.001-10 μM; 72 hours ) inhibits cell proliferation and decreases cancer cell viability in MDA-MB-468, MDA-MB-231, HCT116, Colo-205, and A375. Cell Viability Assay Cell Line: Human breast cancer cells MDA-MB-468 and MDA-MB-231; human colon carcinoma cells HCT116 and Colo-205; human melanoma cell line A375 Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Demonstrated a dose-dependent viability effect with EC50 values of 0.06 μM in MDA-MB-468 cells to 0.45 μM in A375 cells. Western Blot Analysis[1] Cell Line: HCT116 cells Concentration: 0, 0.0007, 0.002, 0.007, 0.02, 0.06, 0.19, 0.56, 1.7, 5 μM Incubation Time: 4 hours Result: Revealed a dose-dependent decrease in the SAE and UBC9 thioester levels.
- 参考文献:
1. He X, et al. Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor. Nat Chem Biol. 2017 Nov;13(11):1164-1171.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.814 ml 9.068 ml 18.135 ml 5 mM 0.363 ml 1.814 ml 3.627 ml 10 mM 0.181 ml 0.907 ml 1.814 ml 50 mM 0.036 ml 0.181 ml 0.363 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)