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MGP-39

Chemical Structure : MGP-39

CAS No.:

MGP-39 (MELK PROTAC MGP-39)

Catalog No.: PC-22852Not For Human Use, Lab Use Only.

MGP-39 is a first-in-class PROTAC degrader targeting maternal embryonic leucine zipper kinase (MELK), induced potent and rapid degradation of MELK in Burkitt lymphoma cell (Dmax=91.6%), and IC50 of 1.8 uM for RAMOS cell line.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MGP-39 is a first-in-class PROTAC degrader targeting maternal embryonic leucine zipper kinase (MELK), induced potent and rapid degradation of MELK in Burkitt lymphoma cell (Dmax=91.6%), and IC50 of 1.8 uM for RAMOS cell line.
MGP-39 potently inhibits the phosphorylation of mTOR in accordance with MELK downregulation.
MGP-39 exhibits the lower cytotoxicity against MDA-MB-231 cells compared to MELK inhibitors JNJ-47117096/MELK-8a.
MGP-39 induces cell cycle arrest and apoptosis in BL cells.

Physicochemical Properties

M.Wt 845.96
Formula C44H51N11O7
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

2-(2,6-dioxopiperidin-3-yl)-5-((2-(2-(2-(4-((4-(4-(4-(3-isobutoxypyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethyl)amino)isoindoline-1,3-dione

References

1. Yonghui Sun, et al. RSC Med Chem. 2024 Jun 4;15(7):2351-2356.

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