IWP 12

Potent PORCN inhibitor; active in vivo CAS# 688353-45-9

IWP 12

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IWP 12: 5mg $115 In Stock
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IWP 12

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Chemical Properties of IWP 12

Cas No. 688353-45-9 SDF Download SDF
PubChem ID 3244448 Appearance Powder
Formula C18H18N4O2S3 M.Wt 418.56
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 2-[(3,6-dimethyl-4-oxo-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(6-methyl-1,3-benzothiazol-2-yl)acetamide
SMILES CC1CC2=C(S1)C(=O)N(C(=N2)SCC(=O)NC3=NC4=C(S3)C=C(C=C4)C)C
Standard InChIKey RBFDSBJDWZOTGR-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H18N4O2S3/c1-9-4-5-11-13(6-9)27-17(19-11)21-14(23)8-25-18-20-12-7-10(2)26-15(12)16(24)22(18)3/h4-6,10H,7-8H2,1-3H3,(H,19,21,23)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of IWP 12

DescriptionPotent inhibitor of Porcupine (PORCN), a membrane-bound O-acyltransferase (MBOAT) (IC50 = 15 nM). Inhibits Wnt/β-catenin and Wnt/planar cell polarity (PCP) signaling pathways. Blocks zebrafish tailfin regeneration in vivo.

IWP 12 Dilution Calculator

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IWP 12 Molarity Calculator

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Preparing Stock Solutions of IWP 12

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3891 mL 11.9457 mL 23.8914 mL 47.7829 mL 59.7286 mL
5 mM 0.4778 mL 2.3891 mL 4.7783 mL 9.5566 mL 11.9457 mL
10 mM 0.2389 mL 1.1946 mL 2.3891 mL 4.7783 mL 5.9729 mL
50 mM 0.0478 mL 0.2389 mL 0.4778 mL 0.9557 mL 1.1946 mL
100 mM 0.0239 mL 0.1195 mL 0.2389 mL 0.4778 mL 0.5973 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on IWP 12

Diverse chemical scaffolds support direct inhibition of the membrane-bound O-acyltransferase porcupine.[Pubmed:22593577]

J Biol Chem. 2012 Jun 29;287(27):23246-54.

Secreted Wnt proteins constitute one of the largest families of intercellular signaling molecules in vertebrates with essential roles in embryonic development and adult tissue homeostasis. The functional redundancy of Wnt genes and the many forms of cellular responses they elicit, including some utilizing the transcriptional co-activator beta-catenin, has limited the ability of classical genetic strategies to uncover their roles in vivo. We had previously identified a chemical compound class termed Inhibitor of Wnt Production (or IWP) that targets Porcupine (Porcn), an acyltransferase catalyzing the addition of fatty acid adducts onto Wnt proteins. Here we demonstrate that diverse chemical structures are able to inhibit Porcn by targeting its putative active site. When deployed in concert with small molecules that modulate the activity of Tankyrase enzymes and glycogen synthase kinase 3 beta (GSK3beta), additional transducers of Wnt/beta-catenin signaling, the IWP compounds reveal an essential role for Wnt protein fatty acylation in eliciting beta-catenin-dependent and -independent forms of Wnt signaling during zebrafish development. This collection of small molecules facilitates rapid dissection of Wnt gene function in vivo by limiting the influence of redundant Wnt gene functions on phenotypic outcomes and enables temporal manipulation of Wnt-mediated signaling in vertebrates.

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