2-chloro-N-(2-(4-methylpiperazin-1-yl)-5-nitrophenyl)benzamide Chemical Properties

Boiling point:

474.4±45.0 °C(Predicted)

Density 

1.360±0.06 g/cm3(Predicted)

pka

11.67±0.70(Predicted)

form 

Solid

color 

Light brown to brown

2-chloro-N-(2-(4-methylpiperazin-1-yl)-5-nitrophenyl)benzamide Usage And Synthesis

Uses

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].

References

[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. DOI:10.1016/j.bmcl.2018.12.035
[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. DOI:10.1021/acs.jmedchem.1c00037