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
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
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EIF4; MNK1
Available Sizes
Frequently Asked Questions
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