| Size | Price | Stock | Qty |
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| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
IRES-C11 targets the internal ribosome entry site (IRES) of the c-MYC gene. c-MYC is a master regulator of cell proliferation, differentiation, and apoptosis that is frequently dysregulated in cancer. IRES-C11 functions by blocking the interaction between heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1), a trans-acting factor required for c-MYC IRES activity, and its corresponding IRES. This inhibits cap-independent translation of c-MYC.
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| ln Vitro |
IRES-C11 inhibits the D1 cyclin When paired with the mTOR PP242 mechanistic target, IRES-dependent initiation and synergistic anti-glioblastoma properties are demonstrated[1].
IRES-C11 (50 nM) inhibits the activity of c-MYC IRES and cyclin D1 significantly. IRES-C11 treatment induces a significant shift in both cyclin D1 and c-MYC mRNA to monosomal/nonribosomal fractions, whereas actin mRNA distribution is unaffected. Reductions in protein levels result from IRES-C11'sinhibitionof cyclin D1 and c-MYC IRES-mediated mRNA translation. The inhibitors bind within the UP1 fragment of heterogeneous nuclear ribonucleoprotein A1, according to mechanistic studies conducted with IRES-C11. In vitro, IRES-C11 specifically inhibits c-MYC IRES-mediated translation. It blocks the interaction of hnRNP A1 with the c-MYC IRES. IRES-C11 does not inhibit BAG-1, XIAP, or p53 IRESes, demonstrating specificity for c-MYC IRES. It is a small-molecule inhibitor that targets cap-independent translation initiation, which is exploited by cancer cells under stress conditions. |
| ln Vivo |
In vivo data for IRES-C11 is not extensively reported in publicly available sources. As a specific inhibitor of c-MYC IRES-mediated translation, the compound has potential applications in animal models of cancer where c-MYC is dysregulated. By blocking cap-independent translation of c-MYC, IRES-C11 could reduce c-MYC protein levels and inhibit tumor growth. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro IRES translation inhibition assay for IRES-C11 uses a bicistronic reporter system where the c-MYC IRES is inserted between two reporter genes. Cells are transfected with the reporter construct and treated with varying concentrations of IRES-C11. IRES-mediated translation is measured by quantifying the activity of the second reporter gene. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for IRES-C11 are conducted in cancer cell lines where c-MYC is dysregulated. Cells are treated with varying concentrations of IRES-C11. c-MYC protein levels are measured by Western blotting. Cell proliferation and viability are measured using standard assays such as MTT or CellTiter-Glo. The specificity of IRES-C11 for c-MYC IRES over other IRESes is confirmed by using control reporter constructs.
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| Animal Protocol |
In vivo studies for IRES-C11 would typically involve xenograft mouse models of cancer. The compound would be administered via intraperitoneal or oral routes. Efficacy would be assessed by measuring tumor growth inhibition and c-MYC protein levels in tumor tissues. However, specific published in vivo protocols for IRES-C11 are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for IRES-C11 is not extensively reported. The compound has a molecular weight of 316.14 g/mol and a molecular formula of C13H11Cl2NO4. It has a boiling point of 415.8±45.0°C at 760 mmHg and a density of 1.5±0.1 g/cm³. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for IRES-C11 is limited. As a research compound, IRES-C11 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. The compound's specificity for c-MYC IRES suggests a favorable off-target profile.
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| References |
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| Additional Infomation |
IRES-C11 (CAS 342416-30-2) is a specific inhibitor of c-MYC IRES-mediated translation. It blocks the interaction between hnRNP A1 and the c-MYC IRES. IRES-C11 does not inhibit BAG-1, XIAP, or p53 IRESes. It has a molecular formula of C13H11Cl2NO4 and a molecular weight of 316.14 g/mol. IRES-C11 is a valuable research tool for studying cap-independent translation and c-MYC regulation in cancer.
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| Molecular Weight |
316.137
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|---|---|
| Exact Mass |
315.006
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| CAS # |
342416-30-2
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| Related CAS # |
342416-30-2
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| PubChem CID |
353999
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| Appearance |
Light yellow to yellow solid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
415.8±45.0 °C at 760 mmHg
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| Flash Point |
205.3±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
2.16
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(Cl)C(=O)N(CC2=CC=C(OC)C=C2OC)C1=O
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| InChi Key |
SYBFPEVCOHEALP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H11Cl2NO4/c1-19-8-4-3-7(9(5-8)20-2)6-16-12(17)10(14)11(15)13(16)18/h3-5H,6H2,1-2H3
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| Chemical Name |
3,4-dichloro-1-[(2,4-dimethoxyphenyl)methyl]pyrrole-2,5-dione
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| Synonyms |
IRES-C11
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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: ~250 mg/mL (~790.8 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 | 3.1632 mL | 15.8158 mL | 31.6316 mL | |
| 5 mM | 0.6326 mL | 3.1632 mL | 6.3263 mL | |
| 10 mM | 0.3163 mL | 1.5816 mL | 3.1632 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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