>>Signaling Pathways>> PROTAC>> PROTAC and Building Blocks>>KB02-SLF

KB02-SLF

Catalog No.GC62186

KB02-SLF는 PROTAC 기반 핵 FKBP12 분해제(분자 접착제)입니다. KB02-SLF는 DCAF16(E3 리가제)을 공유적으로 변형하여 핵 FKBP12 분해를 촉진하고 생물학적 시스템에서 단백질 분해의 내구성을 향상시킬 수 있습니다. SLF는 링커를 통해 유비퀴틴 E3 리가제 리간드 KB02에 결합하여 KB02-SLF를 형성합니다.

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KB02-SLF Chemical Structure

Cas No.: 2384184-40-9

Size 가격 재고 수량
1 mg
US$1,035.00
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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[1].

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[1].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[1].

[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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