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KB02-SLF 

Cat. No.: HY-129610
Handling Instructions

KB02-SLF is an electrophilic PROTAC that promotes the nuclear-localized degradation of protein targets by covalently modifying DCAF16 and can improve the durability of protein degradation in biological systems.

For research use only. We do not sell to patients.

KB02-SLF Chemical Structure

KB02-SLF Chemical Structure

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Description

KB02-SLF is an electrophilic PROTAC that promotes the nuclear-localized degradation of protein targets by covalently modifying DCAF16 and can improve the durability of protein degradation in biological systems[1].

IC50 & Target[1]

Cereblon

 

In Vitro

FLAG-tagged variants of FKBP12 (FLAG-FKBP12) or FKBP12 with a C-terminal nuclear localization sequence (FLAG-FKBP12_NLS) in HEK293T cells to provide cell models for evaluating cytosolic-and nuclear-localized E3-mediated degradation pathways, respectively. KB02-SLF promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72h 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[1].

Molecular Weight

949.52

Formula

C₅₀H₆₅ClN₄O₁₂

SMILES

O=C([[email protected]]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[[email protected]@H](C2=CC=CC(NC(CCOCCOCCNC(COC3=CC4=C(N(C(CCl)=O)CCC4)C=C3)=O)=O)=C2)CCC5=CC=C(OC)C(OC)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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KeyWords:

KB02-SLF | PROTAC | Proteolysis-targeting chimera | Inhibitor | inhibitor | inhibit

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KB02-SLF
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