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Keap1-Nrf2-IN-1 - 98%, high purity , CAS No.2232112-72-8

    Grade & Purity:
  • ≥98%
In stock
Item Number
K648976
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K648976-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
K648976-10mg
10mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$750.90
K648976-50mg
50mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$2,250.90
K648976-100mg
100mg
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$3,350.90
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Basic Description

Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms 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 cytoprotectiv
Storage Temp Store at -80°C
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Product Description

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)

Associated Targets(Human)

KEAP1 Tclin Kelch-like ECH-associated protein 1 (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KEAP1 Tclin Kelch-like ECH-associated protein 1 (1736 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name (2S)-1-[4-[carboxymethyl-(4-methoxyphenyl)sulfonylamino]naphthalen-1-yl]pyrrolidine-2-carboxylic acid
INCHI InChI=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
InChIKey XIIZECUWKNXLCU-QFIPXVFZSA-N
Smiles COC1=CC=C(C=C1)S(=O)(=O)N(CC(=O)O)C2=CC=C(C3=CC=CC=C32)N4CCCC4C(=O)O
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
PubChem CID 138911332
Molecular Weight 484.52

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

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

Solution Calculators

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