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Nobiletin MMP Inhibidor

Cat. No.: S2333

Nobiletin, un flavonoide cítrico aislado de cáscaras de cítricos como la mandarina, que tiene actividades antiinflamatorias y antitumorales.
Nobiletin MMP Inhibidor Chemical Structure

Estructura química

Peso molecular: 402.39

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Control de calidad (Quality Control)

Lote: Pureza: 99.73%
99.73

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad 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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 402.39 Fórmula

C21H22O8

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 478-01-3 Descargar SDF Almacenamiento de soluciones madre

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 80 mg/mL (198.81 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 3 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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.).
Referencias