WDR5-C47 is a highly potent and selective antagonist of WDR5-MLL interaction with an IC50 ~0.3 µM. WDR5-C47 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.
CAS Number: 1422389-91-0
Molecular Weight: 406.84
Chemical Name: 2-chloro-4-fluoro-3-methyl-N-(2-(4-methylpiperazin-1-yl)-5-nitrophenyl)benzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
WDR5-C47 was suggested to be used at 10 µM final concentration in vitro and in cellular assays.
- 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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