WDR5-0103, WDR5 Inhibitor


Catalog No. size PriceQuantity
M60233-2S 2 mg solid $89
M60233-10S 10mg solid $352

Description

Product Information
Molecular Weight: 383.44
Formula: C21H25N3O4
Purity: ≥98%
CAS#: 890190-22-4
Solubility: DMSO up to 100 mM
Chemical Name: methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. It has no effect on a panel of seven other methyltransferases, including SETD7. It binds in the WDR5 peptide-binding pocket and inhibits the catalytic activity of the MLL core complex in vitro. WDR5-0103 is a good chemical probe to demonstrate inhibition of an important protein-protein interaction and form the basis for further development of inhibitors of WDR5-dependent enzymes implicated in MLL-rearranged leukaemias or other cancers.

How to Use:


In vitro:
 WDR5-0103 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

  • 1. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. (2013) Biochem J. 449(1):151-9. 
 



Products are for research use only. Not for human use. 

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