Keap1-Nrf2-IN-1 是一种 Keap1-Nrf2 蛋白-蛋白相互作用抑制剂，对 Keap1 蛋白作用的 IC₅₀ 值为 43 nM。Keap1-Nrf2-IN-1 能激活 Nrf2 调节的细胞保护反应，并对乙酰氨基酚诱导的肝损伤产生拮抗作用。

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.

Solid

IC50: 43 nM (Keap1 protein)

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 (HY-66005)-induced injury in L02 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 weeks female C57BL/6 mice (18-2

Room temperature in continental US; may vary elsewhere.

-80°C

[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

In Vitro: DMSO : 100 mg/mL (206.39 mM; Need ultrasonic)配制储备液