WDR5-0103

WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a K_d of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases^[1][2][3]. In Vitro:WDR5-0103 (5-20 μM; 72 hours) can sensitize ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells to conventional cytotoxic drugs in a concentration-dependent manner in experiments with multiple cell lines^[2].
WDR5-0103 (1-10 μM; 72 hours) does not alter the protein expression of ABCB1 or ABCG2 in multidrug-resistant cancer cells^[2].
WDR5-0103 (10 μM; 48 hours) can significantly restore drug-induced apoptosis in ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells^[2].
In Vivo:WDR5-0103 (2.5 mg/kg; intraperitoneal injection; once a day; for 3 days) can reduce the level of H₃K4me₃, improve cognitive deficits and restore synaptic function in P301S transgenic Tau mice^[3].
WDR5-0103 (2.5 mg/kg; intraperitoneal injection; three times) can reduce the level of H₃K4me₃ in the prefrontal cortex and improve cognitive function in 5xFAD mice^[3].