Keap1-Nrf2-IN-1

未知

Keap1-Nrf2-IN-1

K648976-5mg

5mg

≥98%

-80℃储存

超低温冰袋运输

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. Form:Solid IC50& Target:IC50: 43 nM (Keap1 protein)

Keap1-Nrf2-IN-1 是一种 Keap1（Kelch-like ECH-associated protein 1）-Nrf2（nuclear factor erythroid 2-related factor 2）蛋白-蛋白相互作用抑制剂，对 Keap1 蛋白的 IC 50 为 43 nM。Keap1-Nrf2-IN-1可激活Nrf2调节的细胞保护活性。

2232112-72-8

C24H24N2O7S

484.52 g/mol

138911332

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

(2S)-1-[4-[carboxymethyl-(4-methoxyphenyl)sulfonylamino]naphthalen-1-yl]pyrrolidine-2-carboxylic acid

1S/C24H24N2O7S/c1-33-16-8-10-17(11-9-16)34(31,32)26(15-23(27)28)21-13-12-20(18-5-2-3-6-19(18)21)25-14-4-7-22(25)24(29)30/h2-3,5-6,8-13,22H,4,7,14-15H2,1H3,(H,27,28)(H,29,30)/t22-/m0/s1

XIIZECUWKNXLCU-QFIPXVFZSA-N

COC1=CC=C(C=C1)S(=O)(=O)N(CC(=O)O)C2=CC=C(C3=CC=CC=C32)N4CCCC4C(=O)O

138911332

DMSO : 100 mg/mL (206.39 mM; Need ultrasonic)