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Purity: ≥98%
IWR-1-endo (also known as IWR 1-endo; IWR1; IWR-1) is a potent tankyrase inhibitor of the Wnt pathway with potential antitumor activity. It inhibits tankyrase with an IC50 of 180 nM in L-cells expressing Wnt3A. IWR-1-endo is able to induce Axin2 protein levels and promote β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. IWR-1-endo binds only to the adenosine-binding site. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. IWR-1 inhibits cell proliferation and EMT even in the presence of TNF-α-induced cancer cell stimulation.
| ln Vitro |
IWR-1 and XAV939 have comparable pharmacological actions in vitro and function as reversible inhibitors of the Wnt pathway. IWR-1 interacts with Axin to provide its effect, whereas XAV939 directly binds to TNKS[1]. IWR-1 (10 μM) causes the β-catenin disruption complex to stabilize. When IWR-1 (10 μM) is given to the medium together with MIF, the size of the cell colonies is drastically reduced, indicating that IWR-1 inhibits MIF's stimulating effect on NSPC proliferation in all MIF concentration groups. The proliferation of NSPC is strongly inhibited, dose-dependently, by 2, 5, and 10 μM of IWR-1. MIF's stimulating effect on NSPC development into the neuron lineage is inhibited by IWR-1[2]. The stimulatory action of FSH is dose-dependently inhibited by IWR-1 administration in the presence of the maximal stimulatory dose of FSH (0.5 ng/mL), with > 75% inhibition seen at the maximal inhibitory dose of IWR-1 (1 µM). The FSH-induced suppression of granulosa cell CARTPT mRNA expression is partially reversed by IWR-1 treatment[3].
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| ln Vivo |
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| Animal Protocol |
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| References |
[1]. Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7.
[2]. Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cells through Wnt/β-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20. [3]. Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant Follicle Selection. PLoS One. 2014 Jun 17;9(6):e100201. |
| Molecular Formula |
C25H19N3O3
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| Molecular Weight |
409.44
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| CAS # |
1127442-82-3
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| Related CAS # |
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| SMILES |
O=C1C2([H])C3([H])C([H])=C([H])C([H])(C3([H])[H])C2([H])C(N1C1C([H])=C([H])C(C(N([H])C2=C([H])C([H])=C([H])C3C([H])=C([H])C([H])=NC2=3)=O)=C([H])C=1[H])=O
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| InChi Key |
ZGSXEXBYLJIOGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)
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| Chemical Name |
4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-benzamide
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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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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4424 mL | 12.2118 mL | 24.4236 mL | |
| 5 mM | 0.4885 mL | 2.4424 mL | 4.8847 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4424 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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