JANEX-1
Based on 4 publication(s) in Google Scholar
JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
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- Pureté : 99.63%
- CAS No.: 202475-60-3
- Formule: C16H15N3O3
- Masse moléculaire:297.31
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) JANEX-1
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Customer Validation & Images
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WB
Activité biologique
Description
IC50 & Target
[1]|
JAK3 78 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| L929 | IC50 |
1.7 μM
Compound: JANEX-1
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Inhibition of LPS-induced nitric oxide production in mouse L929 cells assessed as nitrite formation
Inhibition of LPS-induced nitric oxide production in mouse L929 cells assessed as nitrite formation
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[PMID: 18024136] |
| L929 | IC50 |
14.5 μM
Compound: JANEX-1
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Inhibition of LPS-induced TNFalpha production in mouse L929 cells after 4 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse L929 cells after 4 hrs by ELISA
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[PMID: 18024136] |
| Medulloblastoma cell | EC50 |
1.525 μM
Compound: 12
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Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
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[PMID: 17417631] |
| RAW | IC50 |
1 ng/mL
Compound: JANEX-1
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Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 100 ug/mL after 4 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 100 ug/mL after 4 hrs by ELISA
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[PMID: 18024136] |
| RAW | IC50 |
1.4 μM
Compound: JANEX-1
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Inhibition of LPS-induced nitric oxide production in mouse RAW 264.7 cells assessed as nitrite formation
Inhibition of LPS-induced nitric oxide production in mouse RAW 264.7 cells assessed as nitrite formation
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[PMID: 18024136] |
| RAW | IC50 |
124.5 μM
Compound: JANEX-1
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Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells after 4 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells after 4 hrs by ELISA
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[PMID: 18024136] |
| RAW | IC50 |
32 ng/mL
Compound: JANEX-1
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Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 10 ug/mL after 4 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 10 ug/mL after 4 hrs by ELISA
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[PMID: 18024136] |
| RAW | IC50 |
4.8 ng/mL
Compound: JANEX-1
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Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 1 ug/mL after 4 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells at 1 ug/mL after 4 hrs by ELISA
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[PMID: 18024136] |
| Sf21 | IC50 |
2800 nM
Compound: 7
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Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
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[PMID: 26874741] |
| Sf9 | IC50 |
>1000 nM
Compound: WHI-P131
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Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA
Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA
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[PMID: 14593182] |
| T-cell | IC50 |
>10000 nM
Compound: WHI-P131
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Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting
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[PMID: 14593182] |
In Vitro
JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2, the ZAP/SYK family tyrosine kinase SYK, the TEC family tyrosine kinase BTK, the SRC family tyrosine kinase LYN, or the receptor family tyrosine kinase insulin receptor kinase, even at concentrations as high as 350 μM. JANEX-1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19 but not in melanoma (M24-MET) or squamous carcinoma (SQ20B) cells. WHI-P131 inhibits the clonogenic growth of JAK3-positive leukemia cell lines DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60 (but not JAK3-negative BT-20 breast cancer, M24-MET melanoma, or SQ20B squamous carcinoma cell lines) in a concentration-dependent fashion. WHI-P131 inhibits clonogenic growth in a concentration-dependent fashion with EC50s of 24.4 μM for NALM-6 cells and 18.8 μM for DAUDI cells. At 100 μM, WHI-P131 inhibits the in vitro colony formation by these leukemia cell lines by >99%. In contrast, JANEX-1 does not inhibit the clonogenic growth of JAK3-negative M24-MET melanoma or SQ20B squamous carcinoma cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 202475-60-3
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Appearance Solid
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Masse moléculaire 297.31
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Formule C16H15N3O3
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Color White to gray
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SMILES
OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1
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Synonyms
WHI-P131; Jak3 inhibitor I
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Autophagy
2018;14(3):450-464. PMID: 29297752
JANEX-1 purchased from MedChemExpress. Usage Cited in: Autophagy. 2018;14(3):450-464. [Abstract]
Autophagy is induced by IL4 in primary B cells. (A) WT asthma-prone mice were pretreated with the JAK3 inhibitor JANEX-1 before atomized OVAL challenge
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Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (336.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Cell Assay[1]
The following cell lines are used in various biological assays: NALM-6 (pre-B-ALL), LC1;19 (pre-B-ALL), DAUDI (B-ALL), RAMOS (B-ALL), MOLT-3 (T-cell ALL), HL60 (acute myelogenous leukemia), BT-20 (breast cancer), M24-MET (melanoma), SQ20B (squamous cell carcinoma), and PC3 (prostate cancer). These cell lines are maintained in culture. Cells are seeded in six-well tissue culture plates at a density of 50×104 cells/well in a treatment medium containing various concentrations of JANEX-1 (0.1, 0.2, 0.3, 0.4 and 0.5 nM) and incubated for 24-48 h at 37°C in a humidified 5% CO2 atmosphere. Cells are examined for apoptotic changes after treatment with JANEX-1 by the in situ TdT-mediated dUTP end-labeling assay using the ApopTag apoptosis detection kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Pathogen-free 8-week-old male JAK3-/- (129S4-Jak3tm1Ljb) and C57BL/6 J mice are used. Mice are treated with JANEX-1 at a dose of 20 mg/kg (intraperitoneally) at 1 h before ischemia.
Rats[3]
Male Lewis rats are divided into two experimental groups of five and are injected either i.v. via the dorsal vein of the penis or i.p. with a single 3.3 mg/kg bolus dose of JANEX-1. The rats are anesthetized by the methoxyfluran, and blood samples (0.2 mL) are collected from rat tail vein before and at 5, 10, and 30 min and 1, 1.5, 2, 3, 4, and 6 h after i.v. injections or at 5, 10, 15, 30, and 45 min and 1, 1.5, 2, 3, 4, 5, and 7 h after i.p. injections.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sudbeck EA, et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin Cancer Res. 1999 Jun;5(6):1569-82. [Content Brief]
[2]. Oh YB, et al. Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice. Exp Mol Med. 2013 May 17;45:e23 [Content Brief]
[3]. Uckun FM, et al. In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4'hydroxyphenyl)-amino-6,7- dimethoxyquinazoline. Clin Cancer Res. 1999 Oct;5(10):2954-62. [Content Brief]
[4]. Xia F, et al. IL4 (interleukin 4) induces autophagy in B cells leading to exacerbated asthma. Autophagy. 2018;14(3):450-464. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3635 mL | 16.8175 mL | 33.6349 mL | 84.0873 mL |
| 5 mM | 0.6727 mL | 3.3635 mL | 6.7270 mL | 16.8175 mL | |
| 10 mM | 0.3363 mL | 1.6817 mL | 3.3635 mL | 8.4087 mL | |
| 15 mM | 0.2242 mL | 1.1212 mL | 2.2423 mL | 5.6058 mL | |
| 20 mM | 0.1682 mL | 0.8409 mL | 1.6817 mL | 4.2044 mL | |
| 25 mM | 0.1345 mL | 0.6727 mL | 1.3454 mL | 3.3635 mL | |
| 30 mM | 0.1121 mL | 0.5606 mL | 1.1212 mL | 2.8029 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8409 mL | 2.1022 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6727 mL | 1.6817 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5606 mL | 1.4015 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0511 mL | |
| 100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8409 mL |
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