DAPK Degrader

PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC₅₀ of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the MDM2 protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand (HY-179071); blue: CRBN ligand (HY-10984); black: linker (HY-40171)).

TAT-GluN2BCTM is a membrane-permeable DAPK1-targeting peptide. TAT-GluN2BCTM targets active DAPK1 to lysosomes for degradation. TAT-GluN2BCTM protects neurons from oxidative stress and NMDAR-mediated excitotoxicity by knocking down DAPK1. TAT-GluN2BCTM can be used in the study of neuroprotection.

DAPK1 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC DAPK1 Degrader-1 (HY-179055). PROTAC DAPK1 Degrader-1 is a potent LAG-3 PROTAC degrader with neuroprotective activity.