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MM-102, WDR5-MLL1 Antagonist

MM-102, WDR5-MLL1 Antagonist

$129.00
A highly potent and selective inhibitor of the MLL1/WDR5 interaction.
Catalog No. Unit Price Qty
M60166-2s 2mg solid $129.00

Details

Product Information
Molecular Weight: 669.80
Formula: C35H49F2N7O4
Purity: ≥98%
CAS#: 1417329-24-8
Solubility: DMSO up to 100 mM
Chemical Name: (S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

MM-102 is a highly potent and selective inhibitor of the MLL1/WDR5 interaction with an IC50 ~2.9 nM binding affinity to WDR5. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.  MM-102 provides the first proof-of-concept small molecule inhibitor to target the WDR5/MLL1 protein-protein interaction as a novel therapeutic approach for acute leukemia harboring MLL1 fusion proteins.

 

How to Use:

  • In vitro:  MM-102 was suggested to be used at 10-100 µM final concentration in vitro and in cellular assays. 
  • In vivo:  n/a

 

Reference:

  • 1. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. (2013)  J Am Chem Soc. 135(2):669-82.
 

 



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

Description

Details

Product Information
Molecular Weight: 669.80
Formula: C35H49F2N7O4
Purity: ≥98%
CAS#: 1417329-24-8
Solubility: DMSO up to 100 mM
Chemical Name: (S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

MM-102 is a highly potent and selective inhibitor of the MLL1/WDR5 interaction with an IC50 ~2.9 nM binding affinity to WDR5. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.  MM-102 provides the first proof-of-concept small molecule inhibitor to target the WDR5/MLL1 protein-protein interaction as a novel therapeutic approach for acute leukemia harboring MLL1 fusion proteins.

 

How to Use:

  • In vitro:  MM-102 was suggested to be used at 10-100 µM final concentration in vitro and in cellular assays. 
  • In vivo:  n/a

 

Reference:

  • 1. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. (2013)  J Am Chem Soc. 135(2):669-82.
 

 



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

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