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| Targets |
AC50: 3.29 μM (miR-21)[1]
microRNA-21-IN-2 targets microRNA-21 (miR-21), an oncogenic microRNA that regulates multiple target genes involved in cancer progression. miR-21 is overexpressed in many cancer types and promotes cell proliferation, migration, invasion, and metastasis while inhibiting apoptosis. By inhibiting miR-21, the compound may restore the expression of tumor suppressor genes and other miR-21 targets, thereby suppressing cancer cell growth and survival. The compound acts on the Epigenetics pathway. |
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| ln Vitro |
microRNA-21-IN-2 is able to suppress miR-21 activity, with an AC50 of 3.29 μM[1].
microRNA-21-IN-2 is a potential miR-21 inhibitor with an AC50 value of 3.29 μM. The compound can be used for cancer research. As an inhibitor of oncogenic miR-21, it may suppress cancer cell proliferation and induce apoptosis by restoring the expression of miR-21 target genes. However, detailed in vitro activity data beyond the AC50 value are limited. |
| ln Vivo |
In vivo activity data for microRNA-21-IN-2 are limited as the compound is primarily a research tool for in vitro studies. As a miR-21 inhibitor, it may have potential antitumor activity in vivo by suppressing oncogenic miR-21 function and restoring tumor suppressor gene expression. However, detailed in vivo efficacy studies have not been extensively reported. The compound could be used in mouse xenograft models to evaluate its antitumor activity and potential for cancer therapy.
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| Enzyme Assay |
miR-21 inhibition assays are performed using cell-based reporter systems. Cells are transfected with a luciferase reporter construct containing miR-21 binding sites in the 3'UTR. microRNA-21-IN-2 is added at varying concentrations, and luciferase activity is measured to assess miR-21 inhibition. Alternatively, miR-21 levels can be quantified by qPCR after compound treatment. The AC50 value of 3.29 μM is determined from concentration-response curves.
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| Cell Assay |
Cancer cell lines with high miR-21 expression are seeded in multi-well plates and treated with varying concentrations of microRNA-21-IN-2 for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. miR-21 levels are quantified by qPCR. The expression of miR-21 target genes (e.g., PTEN, PDCD4, SPRY1) is analyzed by qPCR or Western blot. Cell proliferation, apoptosis, and migration/invasion assays are performed to assess the functional effects of miR-21 inhibition.
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| Animal Protocol |
In vivo studies with microRNA-21-IN-2 would typically involve administration to tumor-bearing mice in xenograft models. The compound would be administered via intraperitoneal or oral routes at various doses. Tumor volumes would be measured every 2-3 days. miR-21 levels and target gene expression would be measured in tumor tissues to confirm target engagement. However, detailed published in vivo protocols for microRNA-21-IN-2 are limited as it is primarily a research tool.
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| ADME/Pharmacokinetics |
microRNA-21-IN-2 has molecular formula C17H15N3O3S and molecular weight 341.38. The compound is a solid and should be stored at -20°C for long-term stability. It is soluble in DMSO and other organic solvents. The compound is a research-use only reagent for studying miR-21 function in cancer biology.
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| Toxicity/Toxicokinetics |
Toxicological data for microRNA-21-IN-2 are limited as it is a research compound. As a miR-21 inhibitor, potential toxicities would be related to the biological functions of miR-21 in normal tissues. The compound should be handled with appropriate laboratory safety precautions. In cell culture, the compound is typically used at concentrations around its AC50 value (3.29 μM), which are generally well-tolerated in short-term experiments. Standard preclinical safety assessments would be required for any therapeutic development.
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| References |
[1]. Qihong Huang, et al. Microrna modulators and method for identifying and using the same. Patent. US20100196357A1.
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| Additional Infomation |
microRNA-21-IN-2 is a potential miR-21 inhibitor with an AC50 value of 3.29 μM. miR-21 is an oncogenic microRNA that is overexpressed in various cancers and is associated with poor prognosis. By inhibiting miR-21, the compound may have potential for cancer research and therapy. The compound acts on the Epigenetics pathway and is available as a research reagent for studying microRNA function in cancer biology.
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| Molecular Formula |
C17H15N3O3S
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|---|---|
| Molecular Weight |
341.384302377701
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| Exact Mass |
341.083
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| CAS # |
303018-40-8
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| PubChem CID |
1537239
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
509
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=NC(=C1C#N)SCC(=O)NC2=CC3=C(C=C2)OCO3)C
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| InChi Key |
FWGGPUIEAQRLDJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N3O3S/c1-10-5-11(2)19-17(13(10)7-18)24-8-16(21)20-12-3-4-14-15(6-12)23-9-22-14/h3-6H,8-9H2,1-2H3,(H,20,21)
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| Chemical Name |
N-(1,3-benzodioxol-5-yl)-2-(3-cyano-4,6-dimethylpyridin-2-yl)sulfanylacetamide
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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 : 9.09 mg/mL (26.63 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 | 2.9293 mL | 14.6464 mL | 29.2929 mL | |
| 5 mM | 0.5859 mL | 2.9293 mL | 5.8586 mL | |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9293 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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