WDR5-C47, WDR5-MLL (SET1) Antagonist


Catalog No. size PriceQuantity
M60118-2D 10 mM DMSO (0.492 mL) $129
M60118-2S 2mg solid $129
M60118-10S 10mg solid $529

Description

Product Information
Molecular Weight: 406.84
Formula: C19H20ClFN4O3
Purity: ≥98%
CAS#: 1422389-91-0
Solubility: DMSO up to 100 mM
Chemical Name: 2-chloro-4-fluoro-3-methyl-N-(2-(4-methylpiperazin-1-yl)-5-nitrophenyl)benzamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity: 

WDR5-C47 is a highly potent and selective antagonist of WDR5-MLL interaction with an IC50 ~0.3 µM. It was designed based on the structure of the WDR5-MLL complex. The WD40-repeat protein WDR5 plays a critical role in maintaining the integrity of the MLL complex and fully activating its methyltransferase function. The MLL complex, the trithorax-like family of SET1 methyltransferase, catalyzes trimethylation of lysine 4 on histone 3, and they have been widely implicated in various cancers. WDR5-C47 could serve as a tool compound to study functions of SET1-family of human histone methyltransferases and further develop therapeutic drug molecules targeting the WDR5−MLL interaction. 

 

How to Use:

 

  • In vitro:  WDR5-C47 was suggested to be used at 10 µM final concentration in vitro and in cellular assays.
  • In vivo:  n/a

 

 

Reference: 

  • 1. Bolshan Y, et al. Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction.  (2013) ACS Med. Chem. Lett., 4 (3), 353–357.

 


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

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