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Technical Data
| Formula | C16H15N3O3 |
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| Molecular Weight | 297.31 | CAS No. | 202475-60-3 | |
| Solubility (25°C)* | In vitro | DMSO | 5 mg/mL (16.81 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | JANEX-1 (WHI-P131) is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM). | ||
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| Targets |
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| In vitro | JANEX-1 inhibits JAK3 but not JAK1 or JAK2. The ZAP/SYK family tyrosine kinase SYK, TEC family tyrosine kinase Bruton’s tyrosine kinase (BTK), SRC family tyrosine kinase LYN, and receptor family tyrosine kinase insulin receptor kinase (IRK) are not inhibited by JANEX-1[1]. JANEX-1 suppresses IL-1β and IFN-γ-induced phosphorylation of STAT-1, STAT-3, and STAT-5 proteins. JANEX-1 has a potent inhibitory effect on cytokine-induced β-cell damage[2]. |
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| In vivo | JANEX-1 is very well tolerated by mice and monkeys and effective plasma concentrations of JANEX-1 could be achieved at nontoxic dose levels. JANEX-1 suppresses the mitogen and antigen responses of T-cells and attenuates the severity of T-cell-dependent graft-versus-host disease in a bone marrow transplantation model[1]. |
Protocol (from reference)
| Animal Study: |
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References
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Selleck's JANEX-1 has been cited by 3 publications
| JAK3/STAT5 signaling-triggered upregulation of PIK3CD contributes to gastric carcinoma development [ J Cell Commun Signal, 2024, 18(1):e12017] | PubMed: 38545256 |
| Homeostatic cytokines reciprocally modulate the emergence of prenatal effector PLZF+CD4+ T cells in humans [ JCI Insight, 2023, 8(22)e164672] | PubMed: 37856221 |
| JANEX-1 improves acute pulmonary embolism through VEGF and FAK in pulmonary artery smooth muscle cells [ Exp Biol Med (Maywood), 2020, 1535370220942470] | PubMed: 32664806 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.