PROTAC FAK degrader 3

PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM) . PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker) [1].

Product Specifications

UNSPSC

12352005

Target

FAK; PROTACs

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Smiles

O=C1CCC2=C1C(OC3=NC(NC4=CC=C(C=C4OC)C(NC5CCN(CC5)CCCCCCCOC6=C7C(C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=CC=C6)=O)=NC9=C3C=CN9)=CC=C2

Molecular Formula

C48H50N8O9

Molecular Weight

882.96

References & Citations

[1]Wei W, et al. Identification of a Potent and Selective Focal Adhesion Kinase Proteolysis Targeting Chimera: Targeting Noncatalytic Functions of Focal Adhesion Kinase to Facilitate Antitumor Immunity. J Med Chem. 2025 Jul 31.