Home JAK/STAT JAK inhibitor Selective JAK3 inhibitor 1 For research use only.

Selective JAK3 inhibitor 1

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

Selective JAK3 inhibitor 1 Chemical Structure

CAS No. 1443235-95-7

Purity & Quality Control

Batch: S868401 DMSO]70 mg/mL]false]Ethanol]9 mg/mL]false]Water]Insoluble]false Purity: 99.71%
99.71

Selective JAK3 inhibitor 1 Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

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
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
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].

Chemical Information & Solubility

Molecular Weight 350.37 Formula

C19H18N4O3
CAS No. 1443235-95-7 SDF --
Smiles CCOC(=O)C1=CNC2=NC=NC(=C12)C3=CC(=CC=C3)NC(=O)C(=C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 70 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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