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 ; Blue: CRBN ligase ligand (HY-A0003) ; Black: linker (HY-Y1139) ; CRBN + linker: HY-176430

C35H38N6O6S

670.78

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

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

EIF4; MNK1

98.09

DMSO : 4.17 mg/mL (ultrasonic)

-20°C, 3 years (Powder)

Blue Ice