Information Selective JAK3 inhibitor 1 is an irreversibleJAK3inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK. Targets JAK3 (Cell-free assay); JAK1 (Cell-free assay); JAK2 (Cell-free assay) 0.07 nM(Ki); 320 nM(Ki); 740 nM(Ki) In vitro Selective JAK3 inhibitor 1 is a potent inhibitor of JAK3 (IC50 = 0.15 nM) was 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold [interleukin (IL)-2 versus IL-6] or 140-fold [IL-2 versus erythropoietin or granulocyte-macrophage colony-stimulating factor (GMCSF)] selective in cellular reporter assays and >35-fold selective in human peripheral blood mononuclear cell assays (IL-7 versus IL-6 or GMCSF). The compound blocks cytokine signaling through JAK3, but not through other JAK family enzymes. It inhibits IL-7, IL-15, and IL-2 signaling in T cells, but does not inhibit any other cytokine signaling pathways.
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Selective JAK3 inhibitor 1
CAS number：1443235-95-7 molecular formula：C19H18N4O3
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| Chinese alias | - | ||
| English alias | 7H-Pyrrolo[2,3-d]pyrimidine-5-carboxylic acid,4-[3-[(2-methyl-1-oxo-2-propen-1-yl)amino]phenyl]-,ethyl ester | ||
| CAS number | 1443235-95-7 | molecular formula | C19H18N4O3 |
| molecular weight | 350.37 g/mol | Exact mass | ≥99% |
| PSA | 97.000 Ų | logp | 2.959 |
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