JAK3 Inhibitor VIA cell permeable selective inhibitor of JAK3

JAK3 Inhibitor VI (CAS 856436-16-3)

JAK3 Inhibitor VI | CAS 856436-16-3 is rated 5.0 out of 5 by 1.
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Synonym: (3Z)-5-(3-Pyridinyl)-3-(1H-pyrrol-2-ylmethylene)-1,3-dihydro-2H-indol-2-one methanesulfonate
Application: A cell permeable selective inhibitor of JAK3
CAS Number: 856436-16-3
Molecular Weight: 383.42
Molecular Formula: C18H13N3O•CH3SO3H
* Refer to Certificate of Analysis for lot specific data (including water content).
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JAK3 Inhibitor VI is a cell-permeable 3'-pyridyl oxindole compound that acts as a potent inhibitor of JAK3. JAK3 (Janus kinase 3) belongs to the family of non-receptor Janus tyrosine kinases, which regulate a spectrum of cellular functions downstream of activated cytokine receptors in the lympho-hematopoietic system. Immunological stimuli, such as interferons and cytokines, induce recruitment of Stat transcription factors to cytokine receptor-associated JAK3. JAK3 then phosphorylates proximal Stat factors, which subsequently dimerize, translocate to the nucleus and bind to cis elements upstream of target gene promoters to regulate transcription.


References

1. Adams, C., et al. 2003. Bioorg. Med. Chem. Lett. 13: 3105-3110. PMID: 12941344
2. Chen, J.J., et al. 2006. Bioorg. Med. Chem. Lett. 16: 5633-5638. PMID: 16934457

Usage :
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and water (1 mg/ml).
Storage :
Store at 4° C
IC50 :
JAK3: IC50 = 27 nM; IL-2-induced cell proliferation: IC50 = 760 nM (mouse CTLL); IL-2-induced cell proliferation: IC50 = 250 nM (human T-cells)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
16760524
SMILES :
CS(=O)(=O)O.C1=CC(=CN=C1)C2=CC\\3=C(C=C2)NC(=O)/C3=C\\C4=CC=CN4

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Chen Chen, JJ. et al. (PubMed 16934457) described a new class of pyrimidine-based JAK3 inhibitors that showed low nanomolar activity. -SCBT Publication Review
Date published: 2015-05-14
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