WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. It has no effect on a panel of seven other methyltransferases, including SETD7. It binds in the WDR5 peptide-binding pocket and inhibits the catalytic activity of the MLL core complex in vitro. WDR5-0103 is a good chemical probe to demonstrate inhibition of an important protein-protein interaction and form the basis for further development of inhibitors of WDR5-dependent enzymes implicated in MLL-rearranged leukaemias or other cancers.
CAS Number: 890190-22-4
Molecular Weight: 383.44
Chemical Name: methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate
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: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.
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
WDR5-0103 was used at 10 µM final concentration in various in vitro assays.
- Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. (2013) Biochem J. 449(1):151-9.
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