KH-3 (C09-1141-585)

KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC 50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction.In VitroKH-3 (0-100 μM; 48 h; human breast cancer cell lines) blocks HuR function through decrease Bcl-2, Mis2 and XIAP mRNA levels and inhibits breast cancer cells growth in a dose dependent manner. KH-3 (0-10 μM; 0-24 h; MDA-MB-231 and SUM159 cells) inhibits breast cancer cell migration and invasion in a dose dependent manner. KH-3 (0-10 μM; MDA-MB-231 and SUM159 cells) inhibits the interaction between HuR and FOXQ1 mRNA and decreases the amount of HuR protein pulled down by biotinylated ARE FOXQ1 RNA oligomer. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 5 and 10 μM Incubation Time: 48 hours Result: Reduced the protein expression levels of Bcl-2, Msi2 and XIAP.In VivoKH-3 (100 mg/kg; i.p.; three times a week for three weeks; female athymic NCr-nu/nu mice and BALB/c mice) inhibits breast cancer growth and metastasis in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female athymic NCr-nu/nu mice of MDA-MB-231 orthotopic xenograft and BALB/c mice of MDA-MB-231 orthotopic xenograft Dosage: 100 mg/kg Administration: Intraperitoneal injection; three times a week for three weeks Result: Inhibited tumor growth, resulting in 60% tumor regression after three-week treatment and delayed the initiation of pulmonary metastases. Reduced the protein expression levels of HuR targets in tumor tissues as well as the induction of E-cadherin expression.Form:Solid. Specification: 0.98 Molecular Formula: C21H22N2O4S2 Molecular Weight: 430.54 PubChem CID: 45138018 Isomeric SMILES: CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(C=C2)SC(=C3)/C=C/C(=O)NO