WDR5-0103 is a potent and selective small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM). WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5. WD repeat domain 5 (WDR5) plays an important role in various biological functions through the epigenetic regulation of gene transcription.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction.
Li DD, et al. Bioorg Med Chem. 2016 Nov 15;24(22):6109-6118. PMID: 27720555.
Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra G, et al. Biochem J. 2013 Jan 1;449(1):151-9. PMID: 22989411.
|Related Histone Methyltransferase Products|
MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM.
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM.
MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM.
MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.
BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM.
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