1. PROTAC
    Autophagy
    Apoptosis
    Immunology/Inflammation
  2. PROTAC
    FKBP
  3. KB02-SLF

KB02-SLF 

Cat. No.: HY-129610
Handling Instructions

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.

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 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].

IC50 & Target

FKBP12[1]

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-SLFPROTACFKBPProteolysis-targeting chimeraFK506-binding proteinDegradermoleculargluecovalentlymodifyingDCAF16durabilityPROTAC-basedInhibitorinhibitorinhibit

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KB02-SLF
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HY-129610
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