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Cat.nr.S7085
| Gerelateerde doelwitten | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Overig Wnt/beta-catenin Inhibitoren | IWR-1-endo Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 Salinomycin (Procoxacin) FH535 LF3 |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | 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 | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 466.6 | Formule | C22H18N4O2S3 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 686770-61-6 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | 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)
Verwarmd met een waterbad van 50°C;
Geultrasoneerd;
DMF : 12.5 mg/mL Water : Insoluble |
|
In vivo |
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Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Kenmerken |
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 is nuttig in zowel regeneratieve geneeskunde als kankerbestrijdingsinspanningen. Deze verbinding inactiveert Porcn, een membraangebonden O-acyltransferase (MBOAT), en remt selectief de palmitoylering van Wnt. Het blokkeert Wnt-afhankelijke fosforylering van de Lrp6-receptor en Dvl2, en β-catenine accumulatie. |
Referenties |
|
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin |