890190-22-4
Chemical Structure
WDR5-0103
Synonym(s): WD-Repeat Protein 5-0103
- CAS No.: 890190-22-4
- Formula:C21H25N3O4
- Molecular Weight:383.44
IUPAC Name: methyl 3-(3-methoxybenzamido)-4-(4-methylpiperazin-1-yl)benzoate
InChIKey: ZPLBXOVTSNRBFB-UHFFFAOYSA-N
SMILES: O=C(OC)C1=CC=C(N2CCN(C)CC2)C(NC(C3=CC=CC(OC)=C3)=O)=C1
Biological Activity: WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases[1][2][3].
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WDR5-0103 | 99.94% | WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases. | ||||||||||||||||||||
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References
- [1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159. [Content Brief]
- [2]. Wu CP, et al. The WD repeat-containing protein 5 (WDR5) antagonist WDR5-0103 restores the efficacy of cytotoxic drugs in multidrug-resistant cancer cells overexpressing ABCB1 or ABCG2. Biomed Pharmacother. 2022 Oct;154:113663. [Content Brief]
- [3]. Cao Q, et al. Targeting histone K4 trimethylation for treatment of cognitive and synaptic deficits in mouse models of Alzheimer's disease. Sci Adv. 2020 Dec 9;6(50):eabc8096. [Content Brief]
