MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease.
性状
Solid
体外研究(In Vitro)
MS159 (0.5-10 μM, 48 h) can induce the degradation of NSD2 protein in a time- and dose-dependent manner while the induced NSD2 degradation is reversible in 293FT cells. MS159 (2.5 μM, 72 h) can effectively degrade NSD2 as well as IKZF1 and IKZF3 in multiple myeloma cell lines KMS11 and H929 while the degradation of IKZF1/3 is mediated through a ubiquitin-proteasome system (UPS-) and cereblon (CRBN-) dependent mechanism.MS159 (2.5 μM, 8 days) can effectively inhibit the growth of KMS11 and H929 multiple myeloma cells through induced NSD2 degradation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Fanye Meng, et al. Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos. J Med Chem. 2022 Aug 11;65(15):10611-10625.
溶解度数据
In Vitro: DMSO : 50 mg/mL (60.33 mM; Need ultrasonic)配制储备液