PROTAC BET Degrader-18 is a PROTAC targeting BET , with a DC 50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 ( EC 50 = 59.91 nM), and exhibits weak degradation activity against BRD2 . PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc , thereby inducing cell cycle arrest and apoptosis , while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer . (Pink: BRD4 ligand ( HY-184339 ); Blue: Cereblon ligand ( HY-W023573 ); Black: linker).
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Disease Areas > Acute Myeloid Leukemia | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Epigenetics | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Drug Resistance | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Epigenetic Reader Domain | Products > Signaling Pathways > c-Myc | Products > Signaling Pathways > Apoptosis
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