JAK3i

SKU: orb1700305

Description

JAK3i is a selective covalent inhibitor of JAK3 kinase. It potently suppresses a second, delayed wave of STAT5 phosphorylation, which is critical for T cell cycle progression and proliferation. This tool compound is used in vitro and in vivo to study JAK-STAT signaling in immunology and oncology research.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1918238-72-8
• MW: 354.34
• Purity: >99.99% (May vary between batches)
• Formula: C₁₈H₁₅FN₄O₃
• SMILES: C(OCC)(=O)C=1C2=C(N=CN=C2NC1)C3=CC(NC(C=C)=O)=CC=C3F
• Target: JAK
• Solubility: DMSO:10 mg/mL (28.22 mM)

Bioactivity

• Target IC50:
  JAK1:1520 nM|JAK2:8680 nM|JAK3:0.43 nM
• In Vitro:
  We targeted the key downstream IL2R-intermediate JAK 3 using a clinically relevant highly specific JAK3-inhibitor (JAK3i; PF-06651600) that potently inhibited STAT5-phosphorylation in vitro. Low-dose JAK3i combined with cellular and peptide vaccine strategies further decreased tumor load compared with both monotherapies alone. The subsequent phenotype ontology results have revealed JAK3I, PLCG2, and ZEB2 as key hub genes contributing to the inflammation underlying cardiovascular and immune response related phenotypes.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JAK 3i, JAK3, JAK3i, JAK-3i

Compound Identifiers

PubChem CID

118705186