ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC 50/5h of 5 nM. The DC 50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
性状
Solid
IC50 & Target[1][2]
BRD4 5 nM (DC50, 5 hours of treatment) Cereblon
pa
体外研究(In Vitro)
ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3. ZXH-3-26 shows activity exclusively on the first bromodomain of BRD4, and spares degradation of BRD2/3 at concentrations 10 μM. Immunoblot analysis confirms that ZXH-3-26 degrades endogenous BRD4 with comparable efficacy compared to the best pan-BET degrader dBET6, while being inactive on BRD2/3. ZXH-3-26 engages CRBN in a conformation distinct. 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
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.
溶解度数据
In Vitro: DMSO : 200 mg/mL (254.69 mM; Need ultrasonic)配制储备液