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

CAS: 2232112-72-8 Cat. No.: K648976 분자식: C₂₄H₂₄N₂O₇S 분자량: 484.52 PubChem CID: 138911332

GRADE & PURITY ≥98%

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

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)

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

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

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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순수함

≥98%

이름과 식별자

정식 스마일

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

IUPAC Name

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

InChIKey

XIIZECUWKNXLCU-QFIPXVFZSA-N

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

이성체 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

분자량

484.52

관련 대상(인간)

KEAP1 Tclin Kelch-like ECH-associated protein 1 (4 Activities)

Discover Target: KEAP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KEAP1 Tclin Kelch-like ECH-associated protein 1 (1736 Activities)

Discover Target: KEAP1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

관련 대상(비인간)

Mus musculus (284745 Activities)

Explore this target

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)

Discover Target: Nfe2l2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

작용 메커니즘

화학 및 물리적 특성

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

자주 묻는 질문

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2232112-72-8, the molecular formula is C24H24N2O7S, and the molecular weight is 484.52 g/mol. InChIKey XIIZECUWKNXLCU-QFIPXVFZSA-N.

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.