A selective JAK3 inhibitor
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Isomer(s)
44365WHI-P180 (hydrochloride)
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WHI-P131

Item No. 10011246

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
CAS Number
202475-60-3
Synonyms
  • Janex 1
Molecular Formula
C16H15N3O3
Formula Weight
297.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1.5 mg/mlDMSO: 1 mg/mlMethanol: 10 mg/ml
λmax
227, 247, 333 nm
SMILES
COc1cc2c(ncnc2cc1OC)Nc1ccc(O)cc1
InChi Code
InChI=1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-3-5-11(20)6-4-10/h3-9,20H,1-2H3,(H,17,18,19)
InChi Key
HOZUXBLMYUPGPZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $35

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    5 mg

    $147

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    10 mg

    $258

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    25 mg

    $561

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    Product Description

    Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P131 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).1 WHI-P131 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sudbeck, E.A., Liu, X.P., Narla, R.K., et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin. Cancer Res. 5(6), 1569-1582 (1999).

    Product Citations

    Schmidleithner, L., Thabet, Y., Schönfeld, E., et al. Enzymatic activity of HPGD in Treg cells suppresses Tconv cells to maintain adipose tissue homeostasis and prevent metabolic dysfunction. Immunity 50(5), 1232-1248 (2019).