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| 5mg |
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| 10mg |
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| 25mg |
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exo-IWR-1 is an inactive stereoisomer of Endo-IWR-1,and is used as a negative control of IWR-1 (V1351) which is a potent tankyrase inhibitor of the Wnt pathway with potential antitumor activity.
| Targets |
exo-IWR-1 targets the Wnt/β-catenin signaling pathway by stabilizing Axin2, thereby promoting β-catenin degradation, with an EC₅₀ value of 1.2 μM for inhibiting Wnt/β-catenin pathway activity (TOPFlash luciferase assay in Huh7 cells) [2]
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| ln Vitro |
The number of 293T cells infected with the bunyavirus remains unchanged in response to exo-IWR-1 (10 μM) [1]. When cells were pretreated or treated one hour post-infection, exo-IWR-1 had no effect on RVFV MP12-GFP infection [2].
Anti-RVFV activity: exo-IWR-1 (0.1–10 μM) dose-dependently inhibited RVFV replication in Huh7 and Vero cells, with EC₅₀ values of 1.5 μM (Huh7) and 1.8 μM (Vero) (qRT-PCR for viral RNA; viral plaque assay for titer) [2] - Wnt/β-catenin pathway inhibition: 1–5 μM reduced nuclear β-catenin accumulation by 45–78% (immunofluorescence/Western blot) and downregulated Wnt target genes (Axin2, Cyclin D1) by 2.3–3.1-fold (qRT-PCR) in RVFV-infected Huh7 cells [2] - Reduced viral protein expression: 3 μM decreased RVFV N protein levels by 65% (Western blot) and viral progeny release by 72% (plaque assay) [2] - Low cytotoxicity: CC₅₀ > 20 μM in Huh7 and Vero cells; cell viability >90% at concentrations up to 10 μM (MTT assay) [2] - No cross-resistance potential: Did not induce RVFV resistance after 10 serial passages in Huh7 cells treated with sub-EC₅₀ concentrations (0.5 μM) [1] |
| Enzyme Assay |
TOPFlash luciferase assay: Huh7 cells were co-transfected with TOPFlash (Wnt-responsive luciferase reporter plasmid) and Renilla luciferase (internal control plasmid). After 24 hours, cells were pretreated with exo-IWR-1 (0.1–10 μM) for 1 hour, then stimulated with Wnt3a (50 ng/mL) for 16 hours. Luciferase activity was measured, and pathway inhibition rate was calculated; EC₅₀ for pathway inhibition was 1.2 μM [2]
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| Cell Assay |
RVFV replication inhibition assay: Huh7/Vero cells were seeded in 24-well plates, pretreated with exo-IWR-1 (0.1–10 μM) for 1 hour, then infected with RVFV (MOI = 0.1) for 48 hours. Viral RNA was quantified by qRT-PCR; viral titer was determined by plaque assay [2]
- Wnt pathway marker detection: RVFV-infected Huh7 cells were treated with exo-IWR-1 (1–5 μM) for 24 hours. Cells were lysed for Western blot (β-catenin, Axin2, RVFV N protein) or fixed for immunofluorescence (nuclear β-catenin staining with DAPI) [2] - Cytotoxicity assay: Huh7/Vero cells were seeded in 96-well plates, treated with exo-IWR-1 (0.1–50 μM) for 72 hours. MTT reagent was added, and absorbance at 570 nm was measured to calculate cell viability and CC₅₀ [2] - Resistance induction assay: Huh7 cells were infected with RVFV and cultured with exo-IWR-1 (0.5 μM, sub-EC₅₀) for 10 serial passages. Viral replication efficiency was measured by qRT-PCR to assess resistance development [1] |
| References |
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| Additional Infomation |
IWR-1-exo is a dicarboxyimide with an externally bridged phthalimide structure, the nitrogen atom being replaced by a 4-(quinoline-8-ylcarbamoyl)benzoyl group. It is a weak axin stabilizer and an analog of IWR-1-endo. It functions as an axin stabilizer. It is a dicarboxyimide-bridged compound.
exo-IWR-1 is a small molecule inhibitor of the Wnt/β-catenin signaling pathway, derived from IWR-1, with enhanced cell permeability[2]. - Its anti-RVFV mechanism involves stabilizing the Axin2 scaffold protein, promoting the ubiquitination and degradation of β-catenin, thereby blocking the Wnt/β-catenin pathway required for RVFV replication[2]. - It was identified as a potential anti-RVFV drug through genome-wide RNAi screening, which highlighted the dependence of RVFV on the host Wnt/β-catenin signaling pathway[1][2]. - This compound has low cytotoxicity and no obvious RVFV resistance has been observed, making it a promising lead compound for the development of anti-RVFV drugs[1][2]. |
| Molecular Formula |
C25H19N3O3
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|---|---|
| Molecular Weight |
409.43700
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| Exact Mass |
409.142
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| CAS # |
1127442-87-8
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| PubChem CID |
1163034
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
643.9±55.0 °C at 760 mmHg
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| Flash Point |
343.2±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.741
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| LogP |
2.65
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
772
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| Defined Atom Stereocenter Count |
4
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~2 mg/mL (~4.88 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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