Keap1-Nrf2-IN-1

CAS: 2232112-72-8 F: C24H24N2O7S W: 484.52

Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) prot

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Bioactivity	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 IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injury[1].
Target	IC50: 43 nM (Keap1 protein)
Invitro	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[1].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[1].Keap1-Nrf2-IN-1 (1-20 μM; 12 hours) produces cytoprotective effects against Acetaminophen (HY-66005)-induced injury in L02 cells[1]. Western Blot Analysis[1] Cell Line:
In Vivo	Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models[1]. Animal Model:
Name	Keap1-Nrf2-IN-1
CAS	2232112-72-8
Formula	C24H24N2O7S
Molar Mass	484.52
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-80°C
Reference	[1]. Lu MC, et al. Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced H