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Purity: ≥98%
IWP-2 (IWP 2, IWP2) is a novel and potent inhibitor of Wnt processing and secretion (specifically, Porcn-mediated Wnt palmitoylation) with potential antineoplastic activity. It inhibits Wnt with an IC50 of 27 nM in a cell-free assay. IWP-2 showed selective blockage of Porcn-mediated Wnt palmitoylation, and does not affect Wnt/β-catenin in general; also it displays no effect against Wnt-stimulated cellular responses. IWP-2 can decrease MKN28 cell proliferation, migration and invasion, and elevate caspase 3/7 activity. IWP-2 can also downregulate the transcriptional activity of the Wnt/β-catenin signaling pathway and downregulate the expression levels of downstream Wnt/β-catenin target genes in MKN28 cells. IWP-2 may be a potential therapeutic option for gastric cancer.
| ln Vitro |
The tested cell lines' growth was decreased by IWP-2 within a single digit μM range. For A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620, and Capan cells, IWP-2 reduces cell proliferation with EC50s of 8.96 μM, 1.90 μM, 2.33 μM, and 3.86 μM, 4.67 μM, 2.76, respectively. 1.90 μM, 2.05 μM, and 1.90 μM[2]. Panc-1 cells were either left untreated or given 2.33 μM IWP-2 for a 48-hour period. When compared to untreated cells, the peak activity of CK1δ kinase in IWP-2-treated cells was roughly 66% of residual activity. In Panc1 cells, IWP-2 decreases CK1δ activity [2].
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| ln Vivo |
In order to assess the effectiveness of IWP-2 in vivo, C57BL/6 mice were intraperitoneally injected with 200 μL of either free liposomes or IWP-2-liposomes for around two hours, and then a comparable volume of blue dye filling was added. rubber beads or E. Coli DH5α. The uptake of blue beads and E was significantly reduced as a result of IWP-2. Coli as measured over a 2-hour period by CFU in peritoneal lavage cells. Moreover, the related mice's lavage fluid had 2-4 times lower levels of TNF-α and IL-6 than the control values. Even the release of the anti-inflammatory cytokine IL-10 is markedly increased by IWP-2 [3].
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| References |
[1]. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
[2]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. [3]. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5 |
| Molecular Formula |
C22H18N4O2S3
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| Molecular Weight |
466.6
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| CAS # |
686770-61-6
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| Related CAS # |
IWP-2;686770-61-6
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| SMILES |
S1C([H])([H])C([H])([H])C2=C1C(N(C1C([H])=C([H])C([H])=C([H])C=1[H])C(=N2)SC([H])([H])C(N([H])C1=NC2C([H])=C([H])C(C([H])([H])[H])=C([H])C=2S1)=O)=O
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| InChi Key |
WRKPZSMRWPJJDH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18N4O2S3/c1-13-7-8-15-17(11-13)31-21(23-15)25-18(27)12-30-22-24-16-9-10-29-19(16)20(28)26(22)14-5-3-2-4-6-14/h2-8,11H,9-10,12H2,1H3,(H,23,25,27)
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| Chemical Name |
N -(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2- d ]pyrimidin-2-yl)thio]-acetamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1432 mL | 10.7158 mL | 21.4316 mL | |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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