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.