JNJ-1013 is a potent and selective IRAK1 PROTAC degrader. It has IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL FP. It induces apoptosis, increases the expression of cleavaged PARP, and decreases the expression of IRAK1, p-IKBα, and pSTAT3(Tyr705).
- Potent and selective IRAK1 PROTAC degrader
- IRAK1 IC50: 72 nM
- IRAK4 IC50: 443 nM
- VHL FP IC50: 1071 nM
- Induces apoptosis and increases cleaved PARP expression
- Decreases IRAK1, p-IKBα, and pSTAT3(Tyr705) expression
- Degrades IRAK1 protein with a DC50 value of 3 nM in a dose-dependent manner
- Demonstrated decreased IRAK1 expression in HEK293T cells (1.5-10000 nM)