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Chemical Structure : WDR5 WIN site inhibitor 16
Catalog No.: PC-49506Not For Human Use, Lab Use Only.
WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.
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WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.
WDR5 WIN site inhibitor 16 displaced WDR5 from chromatin and repressed mRNA expression of WDR5-bound genes.
WDR5 WIN site inhibitor 16 (0.01-3 uM) induced p53 and p21 protein levels and apoptosis in MV4:11 cells.
WDR5 WIN site inhibitor 16 displaced MYC from chromatin at WDR5-displaced genes.
WDR5 WIN site inhibitor 16 exhibited potent anti-proliferative activity against MYC-driven cancer cells, including CHP-134 (neuroblastoma, wt p53, GI50=0.26 uM) and Ramos (Burkitt's lymphoma, mutant p53, GI50=0.49 uM).
| M.Wt | 514.60 | |
| Formula | C30H31FN4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jianhua Tian, et al. J Med Chem. 2020 Jan 23;63(2):656-675.
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