BD-9136

Overview

BD-9136 is a selective BRD4 PROTAC degrader with a DC 50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3 . BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4 , and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1 . Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer . (Pink: BRD4 ligand ( HY-44103 ); Blue: Cereblon ligand ( HY-103596 ); Black: linker ( HY-168692 )).

Application

Products | Products > Disease Areas > Blood Disease | Products > Disease Areas > Acute Myeloid Leukemia | Products > Disease Areas > Acute Lymphoblastic Leukemia | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Breast Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Epigenetics | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Epigenetic Reader Domain

Product Information

• Catalog No.: HY-149878
• CAS No.: 3037514-38-5
• Molecular Formula: C44H44N10O5S
• Molecular Weight: 824.95
• Purity: 98.81%
• Storage: -20°C, protect from light, stored under nitrogen * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
• Availability: In-stock

Source

Original product source