| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
JAK-IN-11 targets Janus kinases (JAKs), a family of intracellular tyrosine kinases that play a critical role in cytokine signaling. By inhibiting JAKs, it blocks the downstream activation of STAT proteins, thereby modulating inflammatory and immune responses.
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| ln Vitro |
The cytoplasmic protein tyrosine kinases known as JAK kinases consist of JAK1, JAK2, JAK3, and TYK2. In the end, STAT proteins attach to particular DNA sequences found in the promoters of cytokine-responsive genes and function as both transcription factors and signaling molecules. Numerous aberrant immune responses, including allergies, asthma, autoimmune diseases like transplant rejection, rheumatoid arthritis, amyotrophic lateral sclerosis, multiple sclerosis, eye disorders, and hematological and solid diseases, are mediated by JAK/STAT signaling. Malignant tumors, include lymphoma and leukemia [1].
In vitro, JAK-IN-11 demonstrates potent and selective inhibition of JAK kinases. Specific IC50 values are not widely reported in the available literature. |
| ln Vivo |
In vivo, JAK-IN-11 has potential for the treatment of skin disorders such as cutaneous lupus. It is used in research to study the role of JAK signaling in inflammatory and autoimmune diseases.
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| Enzyme Assay |
The in vitro JAK kinase assay involves incubating the enzyme with a peptide substrate and ATP in the presence of varying concentrations of JAK-IN-11. The amount of phosphorylated substrate is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for JAK-IN-11 utilize immune cells stimulated with cytokines to induce JAK-STAT signaling. Cells are treated with the compound, and the phosphorylation of STAT proteins is measured by Western blotting or flow cytometry.
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| Animal Protocol |
In vivo animal experiments for JAK-IN-11 would typically involve models of inflammatory skin diseases, such as the imiquimod-induced psoriasis model or the cutaneous lupus model. The compound would be administered orally or topically, and disease severity would be assessed.
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| ADME/Pharmacokinetics |
JAK-IN-11 has a molecular weight of 483.52 g/mol and is soluble in DMSO. It is typically stored as a powder at -20°C. Its purity is ≥95%.
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| Toxicity/Toxicokinetics |
Toxicological data for JAK-IN-11 are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
Drug Indication
R438 has been investigated for the treatment of autoimmune diseases. Mechanism of Action R438 is a selective Janus tyrosine kinase 3 (JAK3) inhibitor prodrug that is converted into its active metabolite, R333. JAKs are cytoplasmic tyrosine kinases involved in immune system activation and cytokine signaling. They exert their effects upon binding to signal transducers and activators of transcription (STATs). JAK3 is crucial for immune system activation; it is highly expressed in cells and thymocytes and can be induced in T cells and B cells. JAK3 is also present in non-hematopoietic cells, but its function in these cells is currently unclear. JAK3 inhibitors inhibit the development of CD8 memory cells by attenuating the interleukin-7 (IL7) and interleukin-15 (IL-15) pathways, making them a promising drug for the treatment of autoimmune diseases. JAK-IN-11 is a research compound with no clinical approval. It is a valuable tool for studying JAK biology and the role of JAK-STAT signaling in inflammatory and autoimmune diseases. It is used in drug discovery programs to explore the therapeutic potential of JAK inhibitors for the treatment of skin disorders. |
| Molecular Formula |
C23H22FN5O4S
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|---|---|
| Molecular Weight |
483.515286922455
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| Exact Mass |
483.137
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| CAS # |
916742-11-5
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| PubChem CID |
23648971
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.625
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| LogP |
2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
821
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IGLNXKVGKIFNBQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22FN5O4S/c1-4-12-33-18-10-8-16(9-11-18)26-22-19(24)14-25-23(28-22)27-17-7-6-15(3)20(13-17)34(31,32)29-21(30)5-2/h1,6-11,13-14H,5,12H2,2-3H3,(H,29,30)(H2,25,26,27,28)
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| Chemical Name |
N-[5-[[5-fluoro-4-(4-prop-2-ynoxyanilino)pyrimidin-2-yl]amino]-2-methylphenyl]sulfonylpropanamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~125 mg/mL (~258.52 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 | 2.0682 mL | 10.3408 mL | 20.6817 mL | |
| 5 mM | 0.4136 mL | 2.0682 mL | 4.1363 mL | |
| 10 mM | 0.2068 mL | 1.0341 mL | 2.0682 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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