WDR5-0102

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].

Product Specifications

CAS Number

[824960-50-1]

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.