详情描述
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.
Product information
CAS Number: 890190-22-4
Molecular Weight: 383.44
Formula: C21H25N3O4
Chemical Name: methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate
Smiles: CN1CCN(CC1)C1=CC=C(C=C1NC(=O)C1=CC(=CC=C1)OC)C(=O)OC
InChiKey: 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)
Technical Data
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
In Vitro:
WDR5-0103 was used at 10 µM final concentration in various in vitro assays.
References:
- Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. (2013) Biochem J. 449(1):151-9.
Products are for research use only. Not for human use.