Keap1-Nrf2-IN-1 (C09-1141-418)

Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC 50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injuryIn VitroKeap1-Nrf2-IN-1 (compound 35) increases the mRNA level of Nrf2-regulated genes, NEFL2L (encoding Nrf2 protein), HO-1, NQO-1, and GCLM, in L02 cells at a concentration-dependent manner. Keap1-Nrf2-IN-1 (0.1-10 μM; 12 hours) can concentration dependently up-regulate the protein level of Nrf2, heme oxygen-1(HO-1), NAD(P)H dehydrogenase (quinone) 1 (NQO-1), and glutamate-cysteine ligase regulatory subunit (GCLM) in L02 cells. Keap1-Nrf2-IN-1 (1-20 μM; 12 hours) produces cytoprotective effects against Acetaminophen (HY-66005)-induced injury in L02 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: L02 cells Concentration: 0.1 μM, 1 μM, 5 μM, 10 μM Incubation Time: 12 hours Result: Up-regulated the protein levels of Nrf2 and Nrf2 downstream proteins.In VivoKeap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks female C57BL/6 mice (18-20 g) Dosage: 40 mg/kg Administration: Intraperitoneal injection Result: Ameliorated the pathological symptoms in the Acetaminophen (400 mg/kg; i.p.)-induced mouse model of acute liver injury.Form:SolidIC50& Target:IC50: 43 nM (Keap1 protein). Specification: 0.98 Molecular Formula: C24H24N2O7S Molecular Weight: 484.52 PubChem CID: 138911332 Isomeric SMILES: COC1=CC=C(C=C1)S(=O)(=O)N(CC(=O)O)C2=CC=C(C3=CC=CC=C32)N4CCC[C@H]4C(=O)O