PRT3789

Overview

PRT3789 is a selective SMARCA2 PROTAC degrader ( DC 50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase , induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer , endometrial cancer , colorectal cancer , bladder cancer , esophageal cancer , ovarian cancer , and gastric cancer . (Pink: SMARCA2 ligand ( HY-44824 ); Blue: VHL ligand ( HY-159465 ); Black: linker).

Application

Products | Products > Disease Areas > Lung Cancer | Products > Disease Areas > Respiratory Cancer | Products > Disease Areas > Colorectal Cancer | Products > Disease Areas > Digestive System Cancer | Products > Disease Areas > Ovarian Cancer | Products > Disease Areas > Urogenital Cancer | Products > Disease Areas > Non-Small Cell Lung Cancer | Products > Disease Areas > Cancer | Products > Disease Areas > Respiratory Disease | Products > Disease Areas > Digestive System Disease | Products > Disease Areas > Urogenital Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > SWI/SNF Complex

Product Information

• Catalog No.: HY-159607
• CAS No.: 2755761-78-3
• Molecular Formula: C47H58N10O6S
• Molecular Weight: 891.09
• Purity: 98.08%
• Storage: Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: ≥ 2.5 mg/mL (2.81 mM); Clear solution
• Availability: In-stock

Source

Original product source