| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
STAT6-IN-2 directly targets STAT6, inhibiting its tyrosine phosphorylation and subsequent activation. By blocking STAT6 phosphorylation, the compound prevents the transcription factor from dimerizing and translocating to the nucleus, where it would normally activate the expression of genes involved in Th2 cell differentiation and allergic responses. STAT6-IN-2 also inhibits STAT6-induced reporter luciferase activity in 293-EBNA cells, confirming its on-target activity.
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| ln Vitro |
STAT6-IN-2 demonstrates potent inhibition of STAT6 signaling in vitro. It effectively reduces the secretion of eotaxin-3, a key chemokine involved in eosinophil recruitment. In 293-EBNA cells, the compound inhibits STAT6-induced reporter luciferase activity, confirming its ability to block STAT6-mediated transcription. Additionally, STAT6-IN-2 inhibits the tyrosine phosphorylation of STAT6, a critical step in its activation pathway. These activities position STAT6-IN-2 as a useful probe for studying STAT6-dependent immune responses.
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| ln Vivo |
In vivo activity data for STAT6-IN-2 are limited in the available literature. The compound is primarily characterized for its in vitro effects on STAT6 phosphorylation and eotaxin-3 secretion. As a tool compound for studying STAT6 biology, it may have potential applications in animal models of allergic inflammation, such as ovalbumin-induced asthma models, where inhibition of STAT6 could reduce Th2-mediated airway inflammation and hyperresponsiveness. However, specific in vivo efficacy data for STAT6-IN-2 have not been extensively reported.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for STAT6-IN-2 typically involves a STAT6 phosphorylation assay using recombinant STAT6 protein or cell lysates. The compound is incubated with STAT6 in the presence of ATP, and the level of phosphorylated STAT6 is measured using an ELISA or Western blot with phospho-specific antibodies. Inhibition of STAT6 phosphorylation by the compound indicates direct targeting of the STAT6 activation mechanism. Alternatively, a STAT6-DNA binding assay can be performed using an electrophoretic mobility shift assay (EMSA) or a colorimetric ELISA-based DNA-binding assay.
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| Cell Assay |
The in vitro cellular assay for STAT6-IN-2 typically uses 293-EBNA cells transfected with a STAT6-responsive luciferase reporter construct. Cells are treated with varying concentrations of the compound, followed by stimulation with IL-4 to activate STAT6 signaling. Luciferase activity is then measured to quantify STAT6-dependent transcriptional activity. Alternatively, the compound's effect on eotaxin-3 secretion can be assessed in relevant cell lines by treating cells with STAT6-IN-2 and measuring eotaxin-3 levels in the culture supernatant using ELISA. STAT6 tyrosine phosphorylation can also be evaluated by Western blot.
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| Animal Protocol |
In vivo animal studies for STAT6-IN-2 are not extensively documented. For STAT6 inhibitors in general, common in vivo models include ovalbumin-induced asthma models in mice, where compound efficacy is assessed by measuring airway hyperresponsiveness, eosinophil infiltration in bronchoalveolar lavage fluid, and Th2 cytokine levels. However, specific protocols for STAT6-IN-2 in such models have not been reported in the available literature. Researchers should design appropriate experiments based on the compound's properties and the biological question being addressed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for STAT6-IN-2 are not extensively reported in the public domain. The compound is soluble in DMSO at 80 mg/mL (170.37 mM) and can be formulated in 10% DMSO + 90% Corn Oil at 3.3 mg/mL (7.03 mM) for in vivo administration. As a research tool, detailed ADME parameters such as half-life, bioavailability, and clearance have not been thoroughly characterized. Researchers should perform their own pharmacokinetic studies if in vivo application is intended.
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| Toxicity/Toxicokinetics |
Toxicity data for STAT6-IN-2 are not available in the public literature. As with most research compounds, comprehensive toxicological evaluations have not been conducted. The compound is intended for laboratory research use only and should be handled with standard laboratory safety practices. Appropriate personal protective equipment, including gloves and lab coats, should be worn when handling this compound. Refer to the product's safety data sheet for specific handling and disposal instructions.
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| References | |
| Additional Infomation |
STAT6-IN-2 (Compound R-84) is a research tool for studying STAT6 signaling and its role in immune diseases. It inhibits STAT6 tyrosine phosphorylation and reduces eotaxin-3 secretion, a chemokine involved in eosinophil infiltration. The compound is used in cellular assays to investigate STAT6-dependent transcriptional activity. STAT6-IN-2 is not in clinical trials and has not been approved for therapeutic use. It remains an experimental compound for basic research into allergic inflammation and immune regulation. Further studies are needed to explore its potential as a lead compound for drug development.
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| Molecular Formula |
C28H31N5O2
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|---|---|
| Molecular Weight |
469.57804608345
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| Exact Mass |
469.247
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| CAS # |
1355594-85-2
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| PubChem CID |
56950508
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| Appearance |
White to light yellow solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
716
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C(C)C)NC(=O)C1=CC(=CC(=N1)C(=O)NCCC2=CC=CC=N2)C3=CC4=CC=CC=C4N3C
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| InChi Key |
NQCIABFWMPKOJV-LJQANCHMSA-N
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| InChi Code |
InChI=1S/C28H31N5O2/c1-18(2)19(3)31-28(35)24-16-21(26-17-20-9-5-6-11-25(20)33(26)4)15-23(32-24)27(34)30-14-12-22-10-7-8-13-29-22/h5-11,13,15-19H,12,14H2,1-4H3,(H,30,34)(H,31,35)/t19-/m1/s1
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| Chemical Name |
6-N-[(2R)-3-methylbutan-2-yl]-4-(1-methylindol-2-yl)-2-N-(2-pyridin-2-ylethyl)pyridine-2,6-dicarboxamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1296 mL | 10.6478 mL | 21.2956 mL | |
| 5 mM | 0.4259 mL | 2.1296 mL | 4.2591 mL | |
| 10 mM | 0.2130 mL | 1.0648 mL | 2.1296 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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