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Chemical Structure : WDR5 inhibitor 10
Catalog No.: PC-49598Not For Human Use, Lab Use Only.
WDR5 inhibitor 10 is a highly potent, selective and orally active inhibitor of WD repeat domain 5 (WDR5) with TR-FRET Ki value of <0.02 nM, shows potent antiproliferative activity with GI50 of 9.7 nM in MV4:11 cells.
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WDR5 inhibitor 10 is a highly potent, selective and orally active inhibitor of WD repeat domain 5 (WDR5) with TR-FRET Ki value of <0.02 nM, shows potent antiproliferative activity with GI50 of 9.7 nM in MV4:11 cells.
WDR5 inhibitor 10 binds in the WDR5 WIN site.
WDR5 inhibitor 10 (50-150 mg/kg, oral) demonstrated antitumor effects in an MV4:11 subcutaneous tumor xenograft model.
WDR5 inhibitor 10 showed dose-dependent suppression of universal RPG targets of WDR5 (RPL26, RPL32, RPL35, RPS14, and RPS24) transcripts in MV4:11 cells.
WDR5 inhibitor 10 is well-tolerated in rats up to 100 mg/kg BID dose over the 7-d study without serious adverse effects.
| M.Wt | 587.61 | |
| Formula | C31H28F3N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Teuscher KB, et al. Proc Natl Acad Sci U S A. 2023 Jan 3;120(1):e2211297120.
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