1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. WHI-P97

WHI-P97 

Cat. No.: HY-11067 Purity: 99.13%
Handling Instructions

WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.

For research use only. We do not sell to patients.

WHI-P97 Chemical Structure

WHI-P97 Chemical Structure

CAS No. : 211555-05-4

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
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5 mg USD 120 In-stock
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10 mg USD 210 In-stock
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50 mg USD 520 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
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Description

WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo[1].

IC50 & Target[1]

JAK3

11 μM (IC50)

In Vitro

WHI-P97 inhibits 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/FcεRI crosslinking by >90% at low micromolar concentrations[1].
WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD10 is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose[1].
WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t1/2) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t1/2 of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and Cmax are 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC50 values are 58.4 μM and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution are 322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice[1].
WHI-P97 (intraperitoneal injection; 40 mg/kg; 24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mouse model of allergic asthma[1]
Dosage: 40 mg/kg
Administration: intraperitoneal injection; 24 days
Result: Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels.
Molecular Weight

455.10

Formula

C₁₆H₁₃Br₂N₃O₃

CAS No.
SMILES

BrC1=CC(NC2=NC=NC3=CC(OC)=C(OC)C=C32)=CC(Br)=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.88 mg/mL (12.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1973 mL 10.9866 mL 21.9732 mL
5 mM 0.4395 mL 2.1973 mL 4.3946 mL
10 mM 0.2197 mL 1.0987 mL 2.1973 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.59 mg/mL (1.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.59 mg/mL (1.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

WHI-P97JAKJanus kinaseovalbumin-sensitizedairwayovalbumin challengeeosinophil recruitmentInhibitorinhibitorinhibit

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WHI-P97
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