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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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