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MS159

Chemical Structure : MS159

CAS No.:

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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Purity & Documentation Purity: >98% (HPLC)

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

O=C(C1=CC=C(N2)C(OCC2=O)=C1)N(C3CC3)CC4=CC=C(C(NC5=NC=C(OCCCNC(CNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)C=C5)=O)C=C4

References

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

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