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Home > Inhibitors & Agonists > Epigenetics > Histone Methyltransferase (HMTase)

WDR5-0103

  Cat. No.:  DC8662   Featured
Chemical Structure
890190-22-4
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More than 5000 active chemicals with high quality for research!
Field of application
WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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