Stat

STAT inhibitors target signal transducer and activator of transcription (STAT) proteins, mostly STAT3. STAT proteins are latent cytoplasmic transcription factors activated by tyrosine phosphorylation downstream of cytokine receptors and Janus kinases (JAKs). Once phosphorylated, they dimerize, enter the nucleus and regulate gene expression. Constitutively active STAT3 was shown in 1999 to transform cells, which made it a frequent subject of cancer research. Stattic blocks the Src homology 2 (SH2) domain of STAT3 and its dimerization, and S3I-201 was identified as a STAT3 probe by virtual screening. Cryptotanshinone, a diterpenoid quinone from Salvia miltiorrhiza, also inhibits STAT3. Fludarabine, a purine nucleoside analog, is listed for its reported inhibition of STAT1 signaling. Upstream kinase inhibitors are listed in the neighboring JAK category.

2 Items

  • α7 nAchR-JAK2-STAT3 agonist 1
    Cat. No.
    A33244

    α7 nAchR-JAK2-STAT3 agonist 1

    α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses.

    5 mg
    $395.00
    10 mg
    $645.00
    All 5 sizes
  • ML115
    Cat. No.
    A36482

    ML115

    ML115 is a selective agonist of the signal transducer and activator of transcription 3 (STAT3) with an EC50 of 2 nM. It enhances the expression of BCL3, a STAT3-dependent oncogene, while demonstrating inactivity towards related targets such as STAT1, STAT5, and NF-κB. ML115 has been shown to counterbalance the effects of Ginsenoside Rc on cell viability and inflammatory responses in LPS-stimulated H9c2 and RAW264.7 cells, impacting oxidative stress markers. This compound is valuable for investigating mechanisms in breast and prostate cancer research.

    1 mg
    $75.00
    5 mg
    $195.00
    All 8 sizes

2 Items

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