Home JAK/STAT JAK inhibitor JANEX-1

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JANEX-1 JAK inhibitor

Cat.No.S5903

JANEX-1 (WHI-P131) is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).
JANEX-1 JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 297.31

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Quality Control

Batch: S590301 DMSO]5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.76%
99.76

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (16.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 297.31 Formula

C16H15N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 202475-60-3 -- Storage of Stock Solutions

Synonyms WHI-P131 Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)O)OC

Mechanism of Action

Targets/IC50/Ki
JAK3
(Cell-free assay)
78 μM
In vitro

JANEX-1 inhibits JAK3 but not JAK1 or JAK2. The ZAP/SYK family tyrosine kinase SYK, TEC family tyrosine kinase Bruton’s tyrosine kinase (BTK), SRC family tyrosine kinase LYN, and receptor family tyrosine kinase insulin receptor kinase (IRK) are not inhibited by this compound. It suppresses IL-1β and IFN-γ-induced phosphorylation of STAT-1, STAT-3, and STAT-5 proteins. This chemical has a potent inhibitory effect on cytokine-induced β-cell damage.
In vivo

JANEX-1 is very well tolerated by mice and monkeys and effective plasma concentrations of this compound could be achieved at nontoxic dose levels. It suppresses the mitogen and antigen responses of T-cells and attenuates the severity of T-cell-dependent graft-versus-host disease in a bone marrow transplantation model.
References

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