Description
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM). It inhibits the catalytic activity of MLL core complex in in vitro experiments with IC₅₀ of 39 µM. WDR5 is a component of mixed lineage leukemia (MLL) that targets histone-3 and in vitro data shows interaction of WDR5-0103 with MLL inhibits MLL core complex methyltransferase activity. However WDR5-0103 has no effect on other methyltransferases.
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM). It inhibits the catalytic activity of MLL core complex in in vitro experiments with IC₅₀ of 39 µM. WDR5 is a component of mixed lineage leukemia (MLL) that targets histone-3 and in vitro data shows interaction of WDR5-0103 with MLL inhibits MLL core complex methyltransferase activity. However WDR5-0103 has no effect on other methyltransferases.
Alternate Name/Synonyms: 3-[(3-Methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)benzoic acid methyl ester
Appearance: White Solid
Formulation: N/A
CAS Number: 890190-22-4
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₁H₂₅N₃O₄
Molecular Weight: 383.44
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO (>35 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A WD repeat-containing protein 5 (WDR5) antagonist
MDL Number:
PubChem CID: 6457069
SMILES: CN1CCN(CC1)C2=C(C=C(C=C2)C(=O)OC)NC(=O)C3=CC(=CC=C3)OC
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)
InChi Key: ZPLBXOVTSNRBFB-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |