WDR5-0102

• Description:

  WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM) . WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5[1][2].

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319

• Target:

  WDR5

• Type:

  Reference compound

• Related Pathways:

  Epigenetics

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/wdr5-0102.html

• Purity:

  97.07

• Solubility:

  DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=C(C1=C(Cl)C=CC=C1)NC2=CC([N+]([O-])=O)=CC=C2N3CCN(CC3)C

• Molecular Formula:

  C18H19ClN4O3

• Molecular Weight:

  374.82

• Precautions:

  H302, H315, H319

• References & Citations:

  [1]Ye X, et al. The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening. Bioorg Med Chem Lett. 2019 Feb 15;29 (4) :638-645. |[2]Chen X, et al. Targeting WD Repeat-Containing Protein 5 (WDR5) : A Medicinal Chemistry Perspective. J Med Chem. 2021 Aug 12;64 (15) :10537-10556.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, protect from light)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [824960-50-1]