WHI-P97 HCl

SKU: orb1302678

Description

WHI-P97 HCl is a potent, selective JAK3 inhibitor with a Ki of 0.09 µM. It also inhibits EGFR kinase (IC50=2.5 µM) and suppresses the in vitro invasiveness of EGFR-positive cancer cells. This compound is a valuable research tool for studying JAK3 and EGFR signaling pathways in oncology and immunology research.

Research Area

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

Key Properties

• MW: 491.56
• Purity: 98.55% (May vary between batches)
• Formula: C₁₆H₁₄Br₂ClN₃O₃
• SMILES: COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C(=C3)Br)O)Br)OC.Cl
• Target: JAK
• Solubility: DMSO:4.92 mg/mL (10.01 mM)

Bioactivity

• In Vivo:
  WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose. WHI-P97 showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels. Treatment of ovalbumin-sensitized mice with WHI-P97 prevented the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion. Furthermore, WHI-P97 inhibited the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion.
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• In Vitro:
  WHI-P97 is a potent inhibitor of Janus kinase (JAK)-3. Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.Therapeutic WHI-P97 concentrations, which inhibit mast cell leukotriene synthesis in vitro, could easily be achieved in vivo after the i.v. or i.p. administration of a single nontoxic 40 mg/kg bolus dose of WHI-P97.
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Storage & Handling

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

Alternative Names

JAK3, WHIP97 HCl 211555054(free base), WHI-P-97 HCl 211555-05-4(free base), WHI-P97 HCl 211555-05-4(free base), WHI P97 HCl 211555 05 4(free base)

Compound Identifiers

PubChem CID

155977535