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Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E
Remodelin was used at 1-10 µM in vitro and cellular assays
MLN8237 induced polyploidization and expression of mature megakaryocyte markers in acute megakaryocytic leukemia (AMKL) blasts and displayed potent anti-AMKL activity in vivo
and HER2 inhibitor for the treatment of cancer
AI-10-49 - CAS# 1256094-72-0 60268 Blockage of 4EBP1 T36/T45/S65 phosphorylationAI 10 49, CAS No. 1256094 72 0, is an inhibitor that binds the transcription factor fusion CBF SMMHC. AI 10 49, that selectively binds to CBF SMMHC and disrupts its binding to RUNX1. AI 10 49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI 10 49 triggers selective cell death. These data suggest that direct inhibition of the
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