MM-102, WDR5-MLL1 Antagonist


Catalog No. size PriceQuantity
M60166-2S 2mg solid $129
M60166-10S 10mg solid $529

Description

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.

 

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed