KB02-SLF 是一种基于 PROTAC 的核 FKBP12 降解剂 (molecular glue)。KB02-SLF 通过共价修饰 DCAF16 (E3 ligase) 促进 FKBP12 降解，并可以提高生物系统中蛋白质降解的持久性。KB02-SLF 由 SLF 与泛素 E3 连接酶配体 (KB02) 通过 linker 连接而成。

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.

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FKBP12

KB02-SLF (2 μM; 4-72 hours; HEK293T cells) treatment promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72 h time frame.
Cell imaging studies confirms the selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells. KB02-SLF promotes the loss of FKBP12_NLS across a concentration of ~0.5-5μM, but shows varied reductions in activity at higher concentrations. The degradation of FKBP12_NLS induced by KB02-SLF is mediated by DCAF16. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

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)

[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.

In Vitro: DMSO : 100 mg/mL (105.32 mM; Need ultrasonic)配制储备液