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MS159

Chemical Structure : MS159

CAS No.: 3031353-59-7

MS159 (MS 159)

Catalog No.: PC-49208Not For Human Use, Lab Use Only.

MS159 is a first-in-class NSD2 proteolysis targeting chimera (PROTAC) degrader of nuclear receptor binding SET domain protein 2 (NSD2), also effectively degrads CRBN neo-substrates IKZF1 and IKZF3, but not GSPT1.

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Biological Activity

MS159 is a first-in-class NSD2 proteolysis targeting chimera (PROTAC) degrader of nuclear receptor binding SET domain protein 2 (NSD2), also effectively degrads CRBN neo-substrates IKZF1 and IKZF3, but not GSPT1.
MS159 effectively degrades NSD2 in a concentration-, time-, CRBN-, and proteasome-dependent manner.
MS159 is much more effective in suppressing the growth in cancer cells than the parent NSD2 binder UNC6934.
MS159 is bioavailable in mice and is a valuable chemical tool for exploring the roles of NSD2 in health and disease.

Physicochemical Properties

M.Wt 828.839
Formula C43H40N8O10
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
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-cyclopropyl-N-(4-((5-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)propoxy)pyridin-2-yl)carbamoyl)benzyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide

References

1. Meng F, et al. J Med Chem. 2022 Jul 27. doi: 10.1021/acs.jmedchem.2c00807.

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