WHI-P97

Janus kinase (JAK)-3 inhibitor CAS# 211555-05-4

WHI-P97

Catalog No. BCC2056----Order now to get a substantial discount!

Product Name & Size Price Stock
WHI-P97: 5mg $127 In Stock
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Number of papers citing our products

Chemical structure

WHI-P97

3D structure

Chemical Properties of WHI-P97

Cas No. 211555-05-4 SDF Download SDF
PubChem ID 3796 Appearance Powder
Formula C16H13Br2N3O3 M.Wt 455.11
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 5.88 mg/mL (12.92 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
SMILES COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C(=C3)Br)O)Br)OC
Standard InChIKey YVCXQRVVNQMZEI-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H13Br2N3O3/c1-23-13-5-9-12(6-14(13)24-2)19-7-20-16(9)21-8-3-10(17)15(22)11(18)4-8/h3-7,22H,1-2H3,(H,19,20,21)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of WHI-P97

DescriptionWHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 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. 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.

References:
[1]. Ji KA, Yang MS, Jou I, Shong MH, Joe EH.Thrombin induces expression of cytokine-induced SH2 protein (CIS) in rat brain astrocytes: involvement of phospholipase A2, cyclooxygenase, and lipoxygenase.Glia. 2004 Nov 1;48(2):102-11. [2]. Wong WS, Leong KP.Tyrosine kinase inhibitors: a new approach for asthma.Biochim Biophys Acta. 2004 Mar 11;1697(1-2):53-69. [3]. Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, Navara CS, Narla RK.Structure-based design of novel anticancer agents.Curr Cancer Drug Targets. 2001 May;1(1):59-71. [4]. Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.Clin Cancer Res. 1999 Jun;5(6):1569-82.

WHI-P97 Dilution Calculator

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WHI-P97 Molarity Calculator

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Preparing Stock Solutions of WHI-P97

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1973 mL 10.9864 mL 21.9727 mL 43.9454 mL 54.9318 mL
5 mM 0.4395 mL 2.1973 mL 4.3945 mL 8.7891 mL 10.9864 mL
10 mM 0.2197 mL 1.0986 mL 2.1973 mL 4.3945 mL 5.4932 mL
50 mM 0.0439 mL 0.2197 mL 0.4395 mL 0.8789 mL 1.0986 mL
100 mM 0.022 mL 0.1099 mL 0.2197 mL 0.4395 mL 0.5493 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on WHI-P97

WHI-P97 is a rationally designed potent inhibitor of Janus kinase (JAK)-3.

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References on WHI-P97

Treatment of allergic asthma by targeting janus kinase 3-dependent leukotriene synthesis in mast cells with 4-(3', 5'-dibromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline (WHI-P97).[Pubmed:11082424]

J Pharmacol Exp Ther. 2000 Dec;295(3):912-26.

4-(3',5'-Dibromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline (WHI-P97) is a rationally designed 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. 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. 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. Notably, 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. Further development of WHI-P97 may therefore provide the basis for new and effective treatment as well as prevention programs for allergic asthma in clinical settings.

Description

WHI-P97 is a rationally designed potent inhibitor of JAK-3.

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