solo para uso en investigación
Cat. No.S7085
| Dianas relacionadas | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Otros Wnt/beta-catenin Inhibidores | IWR-1-endo Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 Salinomycin (Procoxacin) FH535 LF3 |
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
|---|---|---|---|---|---|---|
| mouse L cells | Function assay | 24 h | Inhibition of porcupine-mediated Wnt signalling in mouse L cells after 24 hrs by SpringerImages-Topflash reporter assay, EC50=30 nM | 23477365 | ||
| HEK293T | Function assay | 22 hrs | Inhibition of porcupine in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs by Super-top flash reporter gene assay, IC50 = 0.157 μM. | 29630366 | ||
| MIAPaCa2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay, EC50 = 1.9 μM. | 29630366 | ||
| SW620 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay, EC50 = 1.9 μM. | 29630366 | ||
| Capan1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay, EC50 = 2.05 μM. | 29630366 | ||
| PANC1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay, EC50 = 2.33 μM. | 29630366 | ||
| HEK293 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, EC50 = 2.76 μM. | 29630366 | ||
| Panc89 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Panc89 cells after 48 hrs by MTT assay, EC50 = 3.86 μM. | 29630366 | ||
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, EC50 = 4.67 μM. | 29630366 | ||
| A818-6 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A818-6 cells after 48 hrs by MTT assay, EC50 = 8.96 μM. | 29630366 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 466.6 | Fórmula | C22H18N4O2S3 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 686770-61-6 | Descargar SDF | Almacenamiento de soluciones madre |
|
|
| Sinónimos | N/A | Smiles | CC1=CC2=C(C=C1)N=C(S2)NC(=O)CSC3=NC4=C(C(=O)N3C5=CC=CC=C5)SCC4 | ||
|
In vitro |
DMSO
: 20 mg/mL
(42.86 mM)
Calentado con baño de agua a 50°C;
Ultrasonido;
DMF : 12.5 mg/mL Water : Insoluble |
|
In vivo |
|||||
Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
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.)
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.
| Características |
Selective inhibitor of Porcn-mediated Wnt secretion.
|
|---|---|
| Targets/IC50/Ki |
Wnt
(Cell-free assay) 27 nM
M82FCK1δ
(Cell-free assay) 40 nM
|
| In vitro |
IWP-2 es útil tanto en medicina regenerativa como en los esfuerzos contra el cáncer. Este compuesto inactiva Porcn, una O-aciltransferasa unida a la membrana (MBOAT), e inhibe selectivamente la palmitoilación de Wnt. Bloquea la fosforilación dependiente de Wnt del receptor Lrp6 y Dvl2, y la acumulación de β-catenina. |
Referencias |
|
| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin |