Molibresib besylate

Overview

Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan- BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT . By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2 . When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer , small-cell lung cancer and various advanced refractory solid tumors.

Application

Products | Products > Disease Areas > Lung Cancer | Products > Disease Areas > Respiratory Cancer | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Small Cell Lung Cancer | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Disease Areas > Acute Myeloid Leukemia | Products > Disease Areas > Multiple Myeloma | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Respiratory Disease | Products > Signaling Pathways > Epigenetics | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Cancer > Cancer Stem Cells | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Epigenetic Reader Domain | Products > Signaling Pathways > ERK

Product Information

• Catalog No.: HY-13032B
• CAS No.: 1895049-20-3
• Molecular Formula: C28H28ClN5O5S
• Molecular Weight: 582.07
• Purity: 97.04%
• Storage: 4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
• Solubility: ≥ 2.67 mg/mL (4.59 mM); Clear solution
• Availability: In-stock

Source

Original product source