WDR5 inhibitor 41

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Chemical Structure : WDR5 inhibitor 41

Catalog No.: PC-38521Not For Human Use, Lab Use Only.

WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.
WDR5 inhibitor 41 is well tolerated in mice by both iv and po dosing and showed no clinical sign of abnormalities suggesting an enhanced safety
profile for the series.

Physicochemical Properties

M.Wt	534.587
Formula	C29H29F3N6O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-7-((1H-imidazol-1-yl)methyl)-2-(cyclopropyl(4-methylpyridin-2-yl)methyl)-5-(1-ethyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-3,4-dihydroisoquinolin-1(2H)-one

References

1. Kevin B. Teuscher, et al. J Med Chem. 2022. DOI: 10.1021/acs.jmedchem.2c00195

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