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Nobiletin MMP Hämmare

Kat.nr.: S2333

Nobiletin, en citrusflavonoid isolerad från citrusskal som i mandarin, som har antiinflammatoriska och antitumör-aktiviteter.
Nobiletin MMP Hämmare Chemical Structure

Kemisk struktur

Molekylvikt: 402.39

Hoppa till

Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.73%
99.73

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer Analystyp Koncentration Inkubationstid Formulering Aktivitetsbeskrivning PMID
MCF-7 MX Function assay Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=4.4μM 21354800
MDCK Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=4.9μM 21354800
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=11.5μM 11743742
SRA 01/04 Function assay 24 hrs Inhibition of TNF-alpha-induced proMMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE analysis, IC50=17μM 21723726
SRA 01/04 Function assay 24 hrs Inhibition of TNFalpha-stimulated pro MMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE based gelatin zymography assay, IC50=17μM 22047798
SRA 01/04 Function assay 24 hrs Inhibition of PMA-induced proMMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE analysis, IC50=20.9μM 21723726
SRA 01/04 Function assay 24 hrs Inhibition of PMA-stimulated pro MMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE based gelatin zymography assay, IC50=20.9μM 22047798
HT-29 Anticancer assay 72 hrs Anticancer activity against human HT-29 cells after 72 hrs by MTT assay, IC50=24μM 19054677
SHSY5Y Function assay 12 hrs Reduction of hydrogen peroxide-induced apoptotic cell death in human SHSY5Y cells assessed as DNA ladder formation after 12 hrs 18282757
SHSY5Y Function assay 30 uM 3 hrs Elevation of phosphorylated ERK level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis 18282757
SHSY5Y Function assay 30 uM 3 hrs Elevation of phosphorylated p38 level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis 18282757
SHSY5Y Function assay 30 uM 3 hrs Elevation of phosphorylated JNk level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis 18282757
ST-13 Function assay 10 uM 11 days Induction of preadipocyte differentiation in mouse ST-13 cells assessed as lipid accumulation at 10 uM within 11 days by oil red-staining relative to control 19268587
ST-13 Function assay 0.1 to 30 uM 11 days Induction of adipocyte differentiation in mouse ST-13 cells assessed as stimulation of adipsin mRNA expression at 0.1 to 30 uM within 11 days by semi-quantitative RT-PCR 19268587
ST-13 Function assay 0.1 to 30 uM 11 days Induction of adipocyte differentiation in mouse ST-13 cells assessed as stimulation of adipocyte P2 mRNA expression at 0.1 to 30 uM within 11 days by semi-quantitative RT-PCR 19268587
ST-13 Function assay 11 days Induction of adipocyte differentiation in mouse ST-13 cells assessed as increase in PPARgamma2 mRNA level after 11 days by semi-quantitative RT-PCR relative to control 19268587
SRA 01/04 Growth inhibition assay 64 uM 4 days Growth inhibition of human SRA 01/04 cells assessed as reduction in PCNA expression at 64 uM after 4 days by Western blot analysis 23199882
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt 402.39 Formel

C21H22O8

Lagring (från mottagningsdatumet)
CAS-nr 478-01-3 Ladda ner SDF Lagring av stamlösningar

Löslighet (Solubility)

In vitro
Batch:

DMSO : 80 mg/mL (198.81 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molaritetsräknare

Massa Koncentration Volym Molekylvikt
Utspädningsräknare Molekylviktsräknare

In vivo
Batch:

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

mg/kg g μL

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH2O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC50/Ki
MMP
In vitro
Nobiletin, a citrus flavonoid isolated from citrus peels like in tangerine, which has anti-inflammatory and anti-tumor activities. This compound, a polymethoxyflavonoid, is identified as an inhibitor of both NO and O 2- generation. It significantly inhibites two skin inflammation induced by double TPA application. It also suppresses the expression of cyclooxygenase-2 and inducible NO synthase proteins and prostaglandin E2 release. This chemical inhibites the tumor-invasive activity of human fibrosarcoma HT-1080 cells in the Matrigel model, not only by suppressing the expression of MMPs but also augmenting TIMP-1 production through interfering the phosphatidylinositol 3-kinase pathway (PI3-K). It may also prevent atherosclerosis at the level of the vascular wall by inhibiting macrophage foam-cell formation.
In vivo
LD50: 780mg/kg (i.g.).
Referenser