WDR5-0103
Product Specifications
UNSPSC 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: 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.
Target Antigen
Histone Methyltransferase
Type
Reference compound
Related Pathways
Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/WDR5-0103.html
Purity
99.93
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
O=C(OC)C1=CC=C(N2CCN(C)CC2)C(NC(C3=CC=CC(OC)=C3)=O)=C1
Molecular Weight
383.44
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-19347/WDR5-0103-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-19347/WDR5-0103-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
890190-22-4
Available Sizes
Curated Selection
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