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Réf. CatalogueS7085
| Cibles apparentées | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Autre Wnt/beta-catenin Inhibiteurs | IWR-1-endo Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 Salinomycin (Procoxacin) FH535 LF3 |
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | 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 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 466.6 | Formule | C22H18N4O2S3 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 686770-61-6 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | 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)
Réchauffé avec un bain-marie à 50°C;
Ultrasonifié;
DMF : 12.5 mg/mL Water : Insoluble |
|
In vivo |
|||||
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Caractéristiques |
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 est utile à la fois en médecine régénérative et dans les efforts anticancéreux. Ce composé inactive Porcn, une O-acyltransférase liée à la membrane (MBOAT), et inhibe sélectivement la palmitoylation de Wnt. Il bloque la phosphorylation dépendante de Wnt du récepteur Lrp6 et de Dvl2, ainsi que l'accumulation de β-caténine. |
Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin |