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Chemical Structure : MS132
Catalog No.: PC-21507Not For Human Use, Lab Use Only.
MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.
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MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.
MS132 shows high binding affinities to both VCB E3 ligase (KD= 534 ± 48 nM) and WDR5 (KD= 122 ± 56 nM) in ITC assays.
MS132 induces WDR5 degradation in a concentration-, time-, and UPS-dependent manner in PDAC cells.
MS132 exhibits antiproliferative activity in multiple PDAC cell lines including MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05, and PANC-1, with GI50 of 4-32 uM.
MS132 has the potential to be used in in vivo animal studies.
| M.Wt | 1016.13 | |
| Formula | C51H57F4N9O7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xufen Yu, et al. J Med Chem. 2023.
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