dFKBP-1,95.03%
产品编号:Bellancom-103634| CAS NO:1799711-22-0| 分子式:C53H64N6O14| 分子量:1009.11
本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,
dFKBP-1
产品介绍 | dFKBP-1 是一种基于 PROTAC 的有效的 FKBP12 降解剂。dFKBP-1 包含 FKBP12 配体 SLF (HY-114872),基于 Thalidomide 的 Cereblon 配体和一个 linker。 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
生物活性 | dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker. | ||||||||||||||||
体外研究 |
dFKBP-1 potently decreases FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. As with dBET1, destabilization of FKBP12 by dFKBP-1 is rescued by pre-treatment with Carfilzomib, MLN4924, free SLF or free Thalidomide. Cereblon (CRBN)-dependent degradation is established using previously published isogenic 293FT cell lines which are wild-type (293FT-WT) or deficient (293FT-CRBN−/−) for CRBN. Treatment of 293FT-WT cells with dFKBP-1 induces potent, dose-dependent degradation of FKBP12, whereas 293FT-CRBN−/− are unaffected. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 | |||||||||||||||||
体内研究 | |||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (99.10 mM; Need ultrasonic) 配制储备液
*
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。 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
参考文献 |