890190-22-4

890190-22-4 structure

Name: WDR5 0103
Chemical Name: Methyl 3-[(3-methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)benz oate
CAS Number: 890190-22-4
Molecular Formula: C₂₁H₂₅N₃O₄
Molecular Weight: 383.441
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2016-06-30 11:10:34
Modify Date: 2024-01-09 18:44:56
WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.IC50 value: 450 nM (Kd)Target: WDR5in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.

Name	Methyl 3-[(3-methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)benz oate
Synonyms	Benzoic acid, 3-[(3-methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)-, methyl ester Methyl 3-[(3-methoxybenzoyl)amino]-4-(4-methylpiperazin-1-yl)benzoate Methyl 3-[(3-methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)benzoate 3-[(3-Methoxybenzoyl)aMino]-4-(4-Methyl-1-piperazinyl)benzoic Acid Methyl Ester WDR5-0103

Description	WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.IC50 value: 450 nM (Kd)Target: WDR5in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.
Related Catalog	Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Cancer
References	[1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.