Chemical Structure : MNK1 PROTAC P11-2
CAS No.:
MNK1 PROTAC P11-2
Catalog No.: PC-24558Not For Human Use, Lab Use Only.
MNK1 PROTAC P11-2 is a first-in-class, selective MNK1-targeting PROTAC degrader with DC50 of 11.92 nM (MV4-11 cells), Dmax>96%, shows remarkable selectivity for MNK1 over MNK2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MNK1 PROTAC P11-2 is a first-in-class, selective MNK1-targeting PROTAC degrader with DC50 of 11.92 nM (MV4-11 cells), Dmax>96%, shows remarkable selectivity for MNK1 over MNK2.
P11-2 rapidly degraded MNK1 at the dose of 300 nM, with a t1/2 value of 3.64 h.
P11-2 exhibited MNK1 degradation activity in other cancer cell lines, including MOLM-13, MM.1S, and MDA-MB-231.
P11-2 significantly decreased both MNK1 and p-eIF4E levels (IC50 = 22.07 nM), demonstrating superior efficacy compared to DS12881479.
P11-2 induced apoptosis, and arrested the cell cycle at the G1 phase.
P11-2 (20 mg/kg) exhibited favorable PK profiles and robust antitumor effects in xenograft mouse model by subcutaneously transplanting MV4–11 cells.
Physicochemical Properties
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M.Wt
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670.79
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Formula
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C35H38N6O6S
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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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1-(7-((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-7-oxoheptanoyl)-N-(5-phenylthiazol-2-yl)piperidine-4-carboxamide
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References
1. Yang Z, et al. J Med Chem. 2025 May 7. doi: 10.1021/acs.jmedchem.5c00062.
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