Home PI3K/Akt/mTOR Antineoplastic and Immunosuppressive Antibiotics Inhibidor Honokiol

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Honokiol Antineoplastic and Immunosuppressive Antibiotics Inhibidor

Cat. No.: S2310

Honokiol es el principio activo del extracto de magnolia que inhibe la fosforilación de Akt y promueve la fosforilación de ERK1/2. Este compuesto provoca la detención de la fase G0/G1, induce la apoptosis y la autofagia a través de la vía de señalización ROS/ERK1/2. Inhibe la infección por el virus de la hepatitis C (VHC). Fase 3.
Honokiol Antineoplastic and Immunosuppressive Antibiotics Inhibidor Chemical Structure

Estructura química

Peso molecular: 266.334

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.96%
99.96

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
human UACC-903 cells Cytotoxicity assay Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay, IC50=5.1 μM
Vero E6 cells Function assay Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=6.5 μM
human UACC-903 cells Cytotoxicity assay Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay, IC50=7.45 μM
human A549 cells Cytotoxicity assay Cytotoxicity against human A549 cells after 72 hrs by MTS assay, IC50=7.75 μM
human CEM cells Cytotoxicity assay Cytotoxicity against human CEM cells, IC50=10.9 μM
HEK293 cells Function assay Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay, EC50=11.8 μM
human A549 cell Cytotoxicity assay 24 h Cytotoxicity against human A549 cells after 24 hrs by MTS assay, IC50=12.51 μM
human HT-29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay, IC50=13.24 μM
human PBM cells Cytotoxicity assay Cytotoxicity against human PBM cells, IC50=16.1 μM
Hep-G2 cells Cytotoxicity assay Cytotoxicity of compound against human liver tumor cell line (Hep-G2) was determined, IC50=16.5 μM
human HepG2 cells Proliferation assay 24 h Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50=16.5 μM
human K562 cells Proliferation assay Antiproliferative activity against human K562 cells by MTT assay, IC50=21.1 μM
Vero cells Cytotoxicity assay Cytotoxicity against Vero cells, IC50=22.5 μM
human A2780 cells Proliferation assay Antiproliferative activity against cisplatin-sensitive human A2780 cells by MTT assay, IC50=30.5 μM
human SPC-A1 cells Proliferation assay Antiproliferative activity against human SPC-A1 cells by MTT assay, IC50=36.1 μM
HUVEC cells Function assay 20 μM 24 h Antimigratory activity against human HUVEC cells at 20 uM after 24 hrs by wound-healing assay
HEK293 cells Function assay 24-48 h Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
human SH-SY5Y cells Function assay 10 μM 30 mins Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of CHP and TBHP-induced cell death at 10 uM incubated for 30 mins prior to challenge measured after 3 hrs by MTT assay
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 266.334 Fórmula

C18H18O2

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 35354-74-6 Descargar SDF Almacenamiento de soluciones madre

Sinónimos NSC 293100 Smiles C=CCC1=CC(=C(C=C1)O)C2=CC(=C(C=C2)O)CC=C

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 53 mg/mL (198.99 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : 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
Akt-phosphorylation
MEK
In vitro

Honokiol shows pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. This compound is effective on inducing apoptosis in SVR angiosarcoma cells. Treatment of SVR cells with this chemical causes decreased phosphorylation of MAP kinase, akt, and c-src. In addition, it potentiates TRAIL-mediated apoptosis, and its cytotoxicity is partially abrogated by neutralizing antibodies to TRAIL. This compound also has direct antiangiogenic activity, in that it blocks the phosphorylation and rac activation due to VEGF-VEGFR2 interactions. It causes apoptosis in CLL cells through activation of caspase 8, followed by caspase 9 and 3 activation. This chemical prevents interleukin-4-mediated survival of CLL cells, and potentiats the cytotoxicity of CB-1348, FaraA, and 2-CdA. It kills myeloma cells from relapsed patients at doses that does not kill PBMCs. Caspase 3, 7, 8, and 9 are induced by this compound treatment, as well as PARP cleavage. It is found to induce apoptosis in the colon cancer cell lines RKO. This chemical potentiates apoptosis, suppresses osteoclastogenesis, and inhibits invasion through modulation of nuclear factor-kappaB activation pathway. It may act as a potent anti-inflammatory agent with multipotential activities due to an inhibitory effect on the PI3K/Akt pathway.

In vivo

Honokiol is highly effective against SVR angiosarcoma in nude mice. This compound inhibits the growth of RKO cells in murine xenografts. It prevents the growth of MDA-MD-231 breast cancer cells in murine xenografts.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/15259066/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16966432/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18158873/
  • [7] https://pubmed.ncbi.nlm.nih.gov/17487375/
  • [8] https://pubmed.ncbi.nlm.nih.gov/15922325/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot p-EGFR / p-AKT / p-STAT3 / p-ERK / p-GSK3α/β / Bax / p-pRb / p-BAD / IκBα / CDK2 / CDK4 / Cyclin D1 p-Lyn / Lyn / p-PI3K
S2310-WB1
27458163
Immunofluorescence Vimentin / Occludin IκBα / NF-κB p65
S2310-IF1
24508063