WDR5-0103

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].

Product Specifications

CAS Number

[890190-22-4]

Product Name Alternative

WD-Repeat Protein 5-0103

UNSPSC

12352005

Hazard Statement

H410

Target

WDR5

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/WDR5-0103.html

Purity

99.94

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(OC)C1=CC=C(N2CCN(C)CC2)C(NC(C3=CC=CC(OC)=C3)=O)=C1

Molecular Formula

C21H25N3O4

Molecular Weight

383.44

Precautions

H410

References & Citations

[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.|[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. |[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.