PROTAC DAPK1 Degrader-1 is a death-associated protein kinase 1 (DAPK1) degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increases MDM2 protein levels and inhibits neuronal apoptosis in ceramide-induced cells. PROTAC DAPK1 Degrader-1 can be used to study neurological disorders such as cerebral ischemia and traumatic brain injury [1]. (Pink: DAPK ligand; Blue: Cereblon ligand; Black: linker ).
In Vitro, PROTAC DAPK1 Degrader-1 (CP1) (0.1-10 μM; 2-24 h) induces time- and dose-dependent degradation of DAPK1 in SH-SY5Y cells, with a DC50 of 119.6 nM[1]. PROTAC DAPK1 Degrader-1 mediates the degradation of DAPK1 in SH-SY5Y cells via the proteasomal pathway without altering the expression of DAPK1 mRNA; it exhibits no cytotoxicity against SH-SY5Y cells[1]. PROTAC DAPK1 Degrader-1 (3-10 μM) upregulates the MDM2 protein level in SH-SY5Y cells, with a significant upregulation at the concentration of 10 μM, which results from the abrogation of the inhibitory effect of DAPK1 on MDM2 stability[1]. PROTAC DAPK1 Degrader-1 inhibits ceramide-induced apoptosis in SH-SY5Y cells and exhibits neuroprotective effects[1].
References:
[1]. Wu X, et al. Design, synthesis, and biological evaluation of death-associated protein kinase 1 PROTACs. Bioorganic chemistry. 2025 Oct;165:109044.
In Vitro, PROTAC DAPK1 Degrader-1 (CP1) (0.1-10 μM; 2-24 h) induces time- and dose-dependent degradation of DAPK1 in SH-SY5Y cells, with a DC50 of 119.6 nM[1]. PROTAC DAPK1 Degrader-1 mediates the degradation of DAPK1 in SH-SY5Y cells via the proteasomal pathway without altering the expression of DAPK1 mRNA; it exhibits no cytotoxicity against SH-SY5Y cells[1]. PROTAC DAPK1 Degrader-1 (3-10 μM) upregulates the MDM2 protein level in SH-SY5Y cells, with a significant upregulation at the concentration of 10 μM, which results from the abrogation of the inhibitory effect of DAPK1 on MDM2 stability[1]. PROTAC DAPK1 Degrader-1 inhibits ceramide-induced apoptosis in SH-SY5Y cells and exhibits neuroprotective effects[1].
References:
[1]. Wu X, et al. Design, synthesis, and biological evaluation of death-associated protein kinase 1 PROTACs. Bioorganic chemistry. 2025 Oct;165:109044.