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
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M.Wt
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845.96
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Formula
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C44H51N11O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Yonghui Sun, et al. RSC Med Chem. 2024 Jun 4;15(7):2351-2356.
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