Synonyms: compound 11 [PMID: 38019706] | MS-132 | XF056-132
Compound class:
Synthetic organic
Comment: MS132 is a von Hippel-Lindau (VHL)-recruiting WDR5 PROTAC degrader [1]. It induces the formation of the WDR5-MS132-VCB (E3 ubiquitin ligase) ternary complex which promotes WDR5 proteasomal degradation. In pancreatic cancer cells, reduction of WDR5 protein disrupts its interactions with partner oncoproteins in its role as a core chromatin-regulatory scaffolding protein, and this produces an antiproliferative effect in these cells.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Bioactivity Comments |
MS132 binds to the von Hippel-Lindau Elongin C-Elongin B (VCB) E3 ligase complex with an affinity (KD) of 534 nM by isothermal titration calorimetry (ITC), and its DC50 is 92 nM in MIA PaCa-2 (pancreatic cancer) cells [1]. |
Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||
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