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 injury In Vitro Keap1-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 -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 Vivo Keap1-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. IC50& Target:IC50: 43 nM (Keap1 protein)
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Keap1-Nrf2-IN-1
CAS number：2232112-72-8(DMSO) molecular formula：C24H24N2O7S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2232112-72-8(DMSO) | molecular formula | C24H24N2O7S |
| molecular weight | 484.52 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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