research use only
Cat.No.S7085
| Related Targets | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Other Wnt/beta-catenin Inhibitors | ICG-001 IWR-1-endo Isoquercitrin Tegatrabetan (BC-2059) SKL2001 BML-284 (Wnt agonist 1) PRI-724 (Foscenvivint) Salinomycin (from Streptomyces albus) FH535 PNU-74654 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | 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 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 20 mg/mL
(42.86 mM)
Warmed with 50°C water bath;
Ultrasonicated;
DMF : 12.5 mg/mL Water : Insoluble |
|
In vivo |
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| Molecular Weight | 466.6 | Formula | C22H18N4O2S3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 686770-61-6 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CC1=CC2=C(C=C1)N=C(S2)NC(=O)CSC3=NC4=C(C(=O)N3C5=CC=CC=C5)SCC4 | ||
| Features |
Selective inhibitor of Porcn-mediated Wnt secretion.
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|---|---|
| Targets/IC50/Ki |
Wnt
(Cell-free assay) 27 nM
M82FCK1δ
(Cell-free assay) 40 nM
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| In vitro |
IWP-2 is useful in both regenerative medicine and anticancer efforts. This compound inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. It blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin |