2. Signaling Pathways
  3. JAK/STAT Signaling
    Stem Cell/Wnt
  4. STAT

STAT

STAT

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STAT is a family of cytoplasmic protein that regulates many aspects of growth, survival and differentiation in cells. The transcription factors of this family are activated by Janus kinase and dysregulation of this pathway is frequently observed in primary tumours and leads to increased angiogenesis, enhanced survival of tumours and immunosuppression. Gene knockout studies have provided evidence that STAT proteins are involved in the development and function of the immune system and play a role in maintaining immune tolerance and tumour surveillance. STAT proteins were originally described as latent cytoplasmic transcription factors that require phosphorylation for nuclear retention. The unphosphorylated STAT proteins shuttle between cytosol and the nucleus waiting for its activation signal. Once the activated transcription factor reaches the nucleus, it binds to consensus DNA-recognition motif called gamma-activated sites (GAS) in the promoter region of cytokine-inducible genes and activates transcription of these genes.

STAT Isoform Specific Products:

STAT Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13919
    Napabucasin
    		Inhibitor 98.85%
    Napabucasin (BBI608) is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
    Napabucasin
  • HY-N0174
    Cryptotanshinone
    		Inhibitor 98.70%
    Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
    Cryptotanshinone
  • HY-101853
    STAT5-IN-1
    		Inhibitor 98.39%
    STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.
    STAT5-IN-1
  • HY-P1061
    Colivelin
    		Activator 99.27%
    Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
    Colivelin
  • HY-12987
    Pimozide
    		Inhibitor 99.91%
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
    Pimozide
  • HY-W063968
    RO8191
    		Activator ≥99.0%
    RO8191 (CDM-3008), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 directly binds to IFNα/β receptor 2 (IFNAR2) and activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon. RO8191 is a cccDNA modulator (CDM) through interferon-like activity and has anti-HBV activity.
    RO8191
  • HY-129602
    SD-36
    		Inhibitor 99.73%
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SD-36
  • HY-W013523
    2-NP
    		Activator 99.89%
    2-NP is a selective enhancer of STAT1 transcription. 2-NP can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells.
    2-NP
  • HY-N0250
    Saikosaponin D
    		Inhibitor 98.76%
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
    Saikosaponin D
  • HY-125731
    Glycodeoxycholic Acid
    		Activator 99.08%
    Glycodeoxycholic Acid is a natural product found in Streptomyces nigricans, Trypanosoma brucei and C. elegans. Glycodeoxycholic Acid induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis.
    Glycodeoxycholic Acid
  • HY-124500
    AC-4-130
    		Inhibitor 99.93%
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
    AC-4-130
  • HY-N0177
    Diosgenin
    		Inhibitor ≥98.0%
    Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57. Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression.
    Diosgenin
  • HY-N1405
    Cucurbitacin I
    		Inhibitor 99.44%
    Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
    Cucurbitacin I
  • HY-N0201
    Atractylenolide I
    		99.94%
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
    Atractylenolide I
  • HY-16975
    SH-4-54
    		Inhibitor 99.45%
    SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.
    SH-4-54
  • HY-B1436
    Nifuroxazide
    		Inhibitor 99.36%
    Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity. Nifuroxazide is an orally active nitrofuran antibiotic.
    Nifuroxazide
  • HY-N0622
    Morusin
    		Inhibitor 99.94%
    Morusin is a prenylated flavonoid isolated from Morus alba Linn. with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
    Morusin
  • HY-126675A
    AS2863619
    		Activator 99.94%
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
    AS2863619
  • HY-100493
    BP-1-102
    		Inhibitor 99.52%
    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
    BP-1-102
  • HY-129603
    SI-109
    		Inhibitor 99.91%
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
    SI-109
Cat. No. Product Name / Synonyms Application Reactivity
STAT Isoform Comparison

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