[CAS NO. 1443235-95-7]  Selective JAK3 inhibitor 1

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PRODUCTS SPECIFICATIONS [1443235-95-7]

Store
Catalog
SLK-S8684
Brand
Selleck
CAS
1443235-95-7

DESCRIPTION [1443235-95-7]

Overview

MDLMFCD31692331
Molecular Weight350.37
Molecular FormulaC19H18N4O3
SMILESO=C(C1=CNC2=NC=NC(C3=CC=CC(NC(C(C)=C)=O)=C3)=C21)OCC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Selective JAK3 inhibitor 1 is an irreversible 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.