PROTAC MNK1 degrader-1

PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety[1]. Pink: MNK1 ligand (HY-176429) ; Blue: CRBN ligase ligand (HY-A0003) ; Black: linker (HY-Y1139) ; CRBN + linker: HY-176430

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Eukaryotic Initiation Factor (eIF) ; MNK; PROTACs

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

98.09

Solubility

DMSO : 4.17 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=CC2=C1CN(C3C(NC(CC3)=O)=O)C2=O)CCCCCC(N4CCC(C(NC5=NC=C(C6=CC=CC=C6)S5)=O)CC4)=O

Molecular Formula

C35H38N6O6S

Molecular Weight

670.78

References & Citations

[1]Yang Z, et al. Discovery of P11-2: A Potent First-in-Class MNK1-Targeting PROTAC Degrader for the Treatment of Cancer. J Med Chem. 2025 May 22; 68 (10) :10092-10110.