research use only
Cat.No.S6745
| Related Targets | JAK TGF-beta/Smad ERK GSK-3 ROCK Hedgehog/Smoothened PKA Secretase STAT Casein Kinase |
|---|---|
| Other Wnt/beta-catenin Inhibitors | IWR-1-endo PRI-724 (Foscenvivint) IWP-2 Tegatrabetan (BC-2059) Isoquercitrin ICG-001 SKL2001 BML-284 Hydrochloride (Wnt agonist 1, AMBMP) PNU-74654 Salinomycin (Procoxacin) |
| Molecular Weight | 434.49 | Formula | C25H26N2O5 |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 664993-53-7 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | COC1=CC=C(C=C1)C2(CCOCC2)CNC(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CO4 | ||
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In vitro |
DMSO
: 87 mg/mL
(200.23 mM)
Ethanol : 4 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Targets/IC50/Ki |
Wnt
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|---|---|
| In vitro |
JW55 inhibits the PARP domain of TNKS1/2, leading to the stabilisation of AXIN2 followed by increased degradation of β-catenin. Wnt3a-induced HEK293 cells containing a transiently transfected ST-Luc (SuperTop-luciferase) reporter show inhibition by this compound with an IC50 value of 470 nmol/L. It decreases auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 μmol/L and 830 nmol/L, respectively. This chemical-mediated inhibition of canonical Wnt signalling results in reduced cell-cycle progression, proliferation, and colony formation in the CRC cell line SW480 in vitro. |
| In vivo |
This compound reduces XWnt8-induced axis duplication in Xenopus embryos and tamoxifen-induced polyposis formation in conditional APC mutant mice. |
References |
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