Art. -Nr.: HY-15508

JANEX-1

Name: JANEX-1
Brand: MedChemExpress
SKU: HY-15508
Price: 60.00 USD
Availability: InStock
Rating: 5 (4 reviews)

(Synonyms: WHI-P131; Jak3 inhibitor I)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated K_i=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC₅₀ of 78 μM), does not inhibit JAK1 and JAK2.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.63%
CAS. Nr.: 202475-60-3
Formel: C₁₆H₁₅N₃O₃
Molecular Weight:297.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JANEX-1 Chemical Structure

CAS. Nr.: 202475-60-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

JAK3

78 μM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
L929	IC₅₀	1.7 μM Compound: JANEX-1	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	[PMID: 18024136]
L929	IC₅₀	14.5 μM Compound: JANEX-1	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	[PMID: 18024136]
Medulloblastoma cell	EC₅₀	1.525 μM Compound: 12	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	[PMID: 17417631]
RAW	IC₅₀	1 ng/mL Compound: JANEX-1	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	[PMID: 18024136]
RAW	IC₅₀	1.4 μM Compound: JANEX-1	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	[PMID: 18024136]
RAW	IC₅₀	124.5 μM Compound: JANEX-1	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	[PMID: 18024136]
RAW	IC₅₀	32 ng/mL Compound: JANEX-1	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	[PMID: 18024136]
RAW	IC₅₀	4.8 ng/mL Compound: JANEX-1	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	[PMID: 18024136]
Sf21	IC₅₀	2800 nM Compound: 7	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	[PMID: 26874741]
Sf9	IC₅₀	>1000 nM Compound: WHI-P131	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	[PMID: 14593182]
T-cell	IC₅₀	>10000 nM Compound: WHI-P131	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	[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

JANEX-1 is administered at doses ranging from 5 to 100 mg/kg. Evaluation of CPK activity revealed a dose-response curve with an effective dose 50 (ED₅₀) value of 7.44 mg/kg. Mice receiving JANEX-1 displayed significantly reduced CPK and LDH levels. In addition, the infarct size of JANEX-1-treated mice (30.16±2.79%) is significantly decreased when compared with I/R-operated mice (65.64±3.76%)^[2]. JANEX-1 (WHI-P131) is absorbed rapidly, and the time to reach the maximum plasma JANEX-1 concentration (t_max) is 24.7±1.7 min. JANEX-1 is rapidly eliminated with an elimination half-life of 45.6±5.5 min. Although the predicted maximum plasma JANEX-1 concentration is 10.5 ± 0.8 μM, which is only half of the C_max following i.v. administration of the same bolus dose, the i.p. bioavailability is 94.6% and the systemic exposure levels (i.e., AUC) are very similar to those observed after i.v. injection (17.1±2.2 μM h versus 18.1±1.2 μM h)^[3].

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

Chemical Information

CAS. Nr. 202475-60-3
Appearance Solid
Molecular Weight 297.31
Formel C₁₆H₁₅N₃O₃
Color White to gray
SMILES

OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1
Synonyms

WHI-P131; Jak3 inhibitor I
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

All WB

Sort by:

Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Autophagy

IL4 (interleukin 4) induces autophagy in B cells leading to exacerbated asthma. [Abstract]

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
Research Square Print

2023 Feb 28.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3635 mL

16.8175 mL

33.6349 mL

5 mM

0.6727 mL

3.3635 mL

6.7270 mL

10 mM

0.3363 mL

1.6817 mL

3.3635 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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.

Animal Administration^[2]^[3]

Mice^[2]
Pathogen-free 8-week-old male JAK3^-/- (129S4-Jak3^tm1Ljb) 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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

JANEX-1

4 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

JANEX-1

Publications Citing Use of MedChemExpress (MCE) JANEX-1

Alle JAK Isoform-spezifische Produkte anzeigen