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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
670.79
|
|
Formula
|
C35H38N6O6S
|
|
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
|
1-(7-((2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-7-oxoheptanoyl)-N-(5-phenylthiazol-2-yl)piperidine-4-carboxamide
|
References
1. Yang Z, et al. J Med Chem. 2025 May 7. doi: 10.1021/acs.jmedchem.5c00062.
Contact Us
sales@probechem.com
