JANEX-1 (Synonyms: WHI-P131; Jak3 inhibitor I)

Name: JANEX-1
Brand: MedChemExpress
SKU: HY-15508
Rating: 5.0 (5 reviews)

Cat. No.: HY-15508 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

JANEX-1 Chemical Structure

CAS No. : 202475-60-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of JANEX-1:

JANEX-1 hydrochloride Get quote

4 Publications Citing Use of MCE JANEX-1

: 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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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

JAK3

78 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
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	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.

Molecular Weight

297.31

Formula

C₁₆H₁₅N₃O₃

CAS No.

202475-60-3

Appearance

Solid

Color

White to gray

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (253 KB) LCMS (263 KB)

Handling Instructions (2659 KB)

References

[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]

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

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

JANEX-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JANEX-1202475-60-3WHI-P131 Jak3 inhibitor IJANEX1JANEX 1JAKJanus kinaseInhibitorinhibitorinhibit

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JANEX-1 (Synonyms: WHI-P131; Jak3 inhibitor I)

Customer Review

Other Forms of JANEX-1:

JANEX-1 Related Antibodies

4 Publications Citing Use of MCE JANEX-1

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

JANEX-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

JANEX-1 Related Classifications

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