Selective JAK3 inhibitor 1

Catalog No.S8684

For research use only.

Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor 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.

Selective JAK3 inhibitor 1 Chemical Structure

CAS No. 1443235-95-7

Purity & Quality Control

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Biological Activity

Description Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor 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 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(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[1].

In vivo

Selective JAK3 inhibitor 1 has a partial effect on reversing inflammation and bone loss in the rat CIA model when administered therapeutically during the inflammatory phase of the model at doses that meet or exceed the exposure required for complete inhibition of the phenotype when dosed prophylactically. It inhibits leukocyte proliferation, but not erythrocyte proliferation in rats. Selective JAK3 inhibitor 1 could fully inhibit the development of inflammation[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 350.37
Formula

C19H18N4O3

CAS No. 1443235-95-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C1=CNC2=NC=NC(=C12)C3=CC(=CC=C3)NC(=O)C(=C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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