WDR5-0103

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [890190-22-4]