Fig. 1 · Structure

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JANEX-1

Cat. No. A15134 CAS 202475-60-3

JAK3 inhibitor

Janex-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 uM); has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.

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Biological Activity

Target & Activity

Target Activity Value
JAK3 IC50 78 μM

Cellular Effect

Cell Line Activity Value Description Reference
L929 IC50 14.5 μM Inhibition of LPS-induced TNFalpha production in mouse L929 cells after 4 hrs by ELISA [PMID: 18024136]
Medulloblastoma cell EC50 1.525 μM Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay [PMID: 17417631]
RAW IC50 1 ng/mL 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 Inhibition of LPS-induced TNFalpha production in mouse RAW 264.7 cells after 4 hrs by ELISA [PMID: 18024136]
RAW IC50 32 ng/mL 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 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 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 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 Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting [PMID: 14593182]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 202475-60-3
Applications JAK3 inhibitor
Formula C16H15N3O3
Molecular Weight 297.31
Synonyms WHI-P131
SMILES
COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)O)OC

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 5 mg/mL (16.81 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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