WDR5-0103|cas: 890190-22-4|DC Chemicals

Cas No.:	890190-22-4
Synonyms:	WD-Repeat Protein 5-0103,WDR5 0103,WDR50103
SMILES:	C(OC)(=O)C1=CC=C(N2CCN(C)CC2)C(NC(=O)C2=CC=CC(OC)=C2)=C1
Formula:	C₂₁H₂₅N₃O₄
M.Wt:	383.44
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
Target:	IC50 value: 450 nM (Kd) Target: WDR5
In 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.
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.

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