KB02-JQ1是一种高选择性的基于PROTAC的BRD4降解剂(molecularglue)，但不降解BRD2或BRD3。KB02-JQ1通过共价修饰DCAF16(E3ligase)促进BRD4降解，并可以提高生物系统中蛋白质降解的持久性。KB02-JQ1由JQ1与泛素E3连接酶配体(KB02)通过linker连接而成。
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1].
KB02-JQ1 (5-40 μM; 24 hours; HEK293T cells) treatment shows concentration-dependent degradation of endogenous BRD4 in HEK293T cells[1]. Western Blot Analysis[1] Cell Line: HEK293T cells
[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.
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