PROTAC HPK1 Degrader-4

PROTAC HPK1 Degrader-4 (compound E3) is a selective and orally active PROTAC HPK1 degrader with a DC50 of 3.16 nM. PROTAC HPK1 Degrader-4 demonstrates >1000-fold selectivity over GLK. PROTAC HPK1 Degrader-4 promotes immune activation. PROTAC HPK1 Degrader-4 can be used for the study of colon cancer and lymphoma (Pink: ligand for target protein (HY-174355) ; Blue: ligand for E3 ligase CRBN (HY-45808) ; Black: Linker (HY-174356) ; Target protein ligand-linker Conjugate (HY-174357) ) [1].

Product Specifications

UNSPSC

12352005

Target

MAP4K; PROTACs

Related Pathways

MAPK/ERK Pathway; PROTAC

Field of Research

Cancer

Smiles

O=C1N(C(C2=CC(N3CC(C3)CN4CC=C(CC4)C5=C(C=C(C=C5C)C6=NC7=C(N=C6)NC=C7C8=CC(C)=C(C=C8)C(N(C)C)=O)C)=CC=C21)=O)C9C(NC(CC9)=O)=O

Molecular Formula

C46H46N8O5

Molecular Weight

790.91

References & Citations

[1]Wu M, et al. Discovery of a New and Selective HPK1 PROTAC for Enhancing Tumor Immunotherapy through Eliminating GLK Degradation. J Med Chem. 2025 Jun 12;68 (11) :10800-10822.