DATASHEET
Formulation
Powder
Storage:
Powder: 4C for 1 year, -20C for 3 years. DMSO: 4C for 3 month.
Product Information:
Molecular Weight: 383.44
Formula: C21 H25 N3 O4
CAS Number: 890190-22-4
InChi Key: ZPLBXOVTSNRBFB-UHFFFAOYSA-N
InChi: InChI=1S/C21H25N3O4/c1-23-9-11-24(12-10-23)19-8-7-16(21(26)28-3)14-18(19)22-20(25)15-5-4-6-17(13-15)27-2/h4-8,13-14H,9-12H2,1-3H3,(H,22,25)
Smiles: CN1CCN(CC1)C1C=CC(=CC=1NC(=O)C1=CC(=CC=C1)OC)C(=O)OC
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
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.