| Name | WHI-P97 HCl |
| Description | WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 4.92 mg/mL (10.01 mM), Sonication is recommended.
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| Keywords | WHI-P97 HCl 211555-05-4(free base) | WHI-P-97 HCl 211555-05-4(free base) | WHIP97 HCl 211555054(free base) | WHI P97 HCl 211555 05 4(free base) | JAK3 |
| Inhibitors Related | Delgocitinib | Ruxolitinib | Atinvicitinib | Tofacitinib Citrate | Resveratrol | 2-(1,8-naphthyridin-2-yl)phenol | Filgotinib | JAK-IN-10 | Tofacitinib | 2,4,5-Trimethoxybenzoic acid | Lentinan | Raspberry ketone glucoside |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
