IKK-β Degrader

Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.

PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).

PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC₅₀ = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer.