Competitive activity-based protein profiling of LF-268 target engagement in live HCT-116 cells using a click handle-derivatized RAF inhibitor probe
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ABSTRACT: Activity-based protein profiling using 268-TCO, a trans-cyclooctene (TCO)-derivatized analogue of the pan-RAF DFG-out inhibitor LF-268, to characterize intracellular target engagement in live HCT-116 (mutant KRAS/WT RAF) cells. Cells were pre-treated with LF-268 (5 µM) or DMSO as competitor, followed by treatment with 268-TCO probe. After lysis, probe-bound protein complexes were captured via click chemistry using tetrazine (Tz)-coupled sepharose beads. Enriched proteins were identified and quantified by label-free LC-MS/MS.
INSTRUMENT(S):
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): Colon
SUBMITTER:
Daniel Brush
LAB HEAD: Dustin James Maly
PROVIDER: PXD075291 | Pride | 2026-04-20
REPOSITORIES: Pride
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