MS159 是一种有效的核受体结合 SET 结构域蛋白 2 (NSD2)PROTAC降解剂。MS159 可以抑制肿瘤细胞的生长。MS159 是一种探索 NSD2 在健康和疾病中作用的有效化学工具。
生物活性 | 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[1].
|
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[1]. 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[1]. MS159 (2.5 μM, 8 days) can effectively inhibit the growth of KMS11 and H929 multiple myeloma cells through induced NSD2 degradation[1].
Western Blot Analysis[1] Cell Line: | 293FT cells | Concentration: | 0.5-10 μM | Incubation Time: | 0-72 hours | Result: | Resulted in binding affinity for the NSD2-PWWP1 structural domain with a Kdvalue of 1.1 μM, and induced degradation of NSD2 with the DC50value of 5.2 μM after 48 hours. |
|
分子量 | |
性状 | |
Formula | |
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) |
溶解性数据 | In Vitro: DMSO : 50 mg/mL(60.33 mM;Need ultrasonic) 配制储备液 1 mM | 1.2065 mL | 6.0326 mL | 12.0652 mL | 5 mM | 0.2413 mL | 1.2065 mL | 2.4130 mL | 10 mM | 0.1207 mL | 0.6033 mL | 1.2065 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |