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Chemical Structure| 202475-60-3 Chemical Structure| 202475-60-3

Structure of JANEX-1
CAS No.: 202475-60-3

Chemical Structure| 202475-60-3

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

Synonyms: Jak3 inhibitor I; WHI-P131; WHI-P131, WHI P-131, WHI P131, Janex 1

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Product Details of JANEX-1

CAS No. :202475-60-3
Formula : C16H15N3O3
M.W : 297.31
SMILES Code : OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1
Synonyms :
Jak3 inhibitor I; WHI-P131; WHI-P131, WHI P-131, WHI P131, Janex 1
MDL No. :MFCD01862614
InChI Key :HOZUXBLMYUPGPZ-UHFFFAOYSA-N
Pubchem ID :3794

Safety of JANEX-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of JANEX-1

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NOD CD4+ T cells 1.5, 3 and 6 μg/ml 72 hours After long-term culturing, CD4+ T cells exposed to WHI-P131 showed comparable viability to controls and exhibited resistance to the proapoptotic effect of WHI-P131. PMC4012866
BMMCs (Jak3-deficient mice) 3, 10, 30 μM 15 minutes Inhibited antigen-induced degranulation and MAPK phosphorylation PMC1576194
BMMCs (wild-type mice) 3, 10, 30 μM 15 minutes Inhibited antigen-induced degranulation and MAPK phosphorylation PMC1576194
RBL-2H3 cells 3, 10, 30 μM 15 minutes Inhibited antigen-induced degranulation and MAPK phosphorylation PMC1576194
Jak3-/- bone marrow cells 0–1000 ng/ml 2 hours To evaluate the chemotactic response of Jak3-deficient bone marrow cells to CCL25 and CXCL12. Results showed significantly reduced chemotactic responses to CCL25 and CXCL12 in Jak3-deficient bone marrow cells. PMC1782482
Jak3-/- thymocytes 0–500 ng/ml 2 hours To evaluate the chemotactic response of Jak3-deficient thymocytes to CCL25 and CXCL12. Results showed significantly reduced chemotactic responses to CCL25 and CXCL12 in Jak3-deficient thymocytes. PMC1782482

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD mice Prediabetic NOD mice Intraperitoneal injection 75 mg/kg/day Twice daily for 10 days In vivo treatment with WHI-P131 did not affect the frequency and number of CD4+FoxP3+ Tregs but increased the numbers of CD4+FoxP3?TGF-β-secreting T cells. PMC4012866
Mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 20 mg/kg Single dose, 1 hour before ischemia Reduced infarct size, improved myocardial function, reduced myocardial apoptosis and inflammatory cell infiltration PMC3674406

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.82mL

3.36mL

1.68mL

33.63mL

6.73mL

3.36mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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