KHS101 is a small molecule differentiator of neuronal differentiation: TACC3 binder.
KHS101 is a small molecule that drives neuronal differentiation of hippocampal neuronal progenitor cells (NPC). Treatment of NPCs with KHS101 induces expression of the neurogenic transcription factor NeuroD and the neuronal marker Tuj1, and exhibit neuronal morphology and spiking activity (EC50 1 uM). KHS101 binds tightly to TACC3, which is a structural component of the centrosome and mitotic spindle apparatus. TACC3 loss of function studies in mice and stem cells suggest that TACC3 controls progenitor cell expansion and terminal differentiation during development.
Journal of molecular biology, 429(2), 280-294 (2016-12-14)
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (TK) that-once activated upon ligand binding-leads to receptor dimerization, recruitment of protein complexes, and activation of multiple signaling cascades. The EGFR is frequently overexpressed or mutated in various cancers
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