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

STAT

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.

Cat. No. 상품명 효과 Purity Chemical Structure
  • HY-175542
    KB-15
    Inhibitor
    KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.
    KB-15
  • HY-12987S2
    Pimozide-d4-1
    Inhibitor
    Pimozide-d4-1 is the deuterium labeled Pimozide. 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-d<sub>4</sub>-1
  • HY-155807
    DPP
    Inhibitor
    DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety.
    DPP
  • HY-184162
    HSP110-IN-1
    Inhibitor
    HSP110-IN-1 is a HSP110 inhibitor. HSP110-IN-1 binds to HSP110, inhibits the activity of STAT3, and downregulates the expression of downstream genes VEGF, MMP7 and MMP9. HSP110-IN-1 abrogates IL-6-induced epithelial-mesenchymal transition and inhibits the proliferation of colorectal cancer cells. HSP110-IN-1 remodels the tumor microenvironment by inducing a pro-inflammatory phenotype, regulates macrophages, induces PD-L1 expression, and enhances anti-PD-L1 antibody-mediated tumor regression. HSP110-IN-1 can be used in studies related to colorectal cancer.
    HSP110-IN-1
  • HY-178996
    FLT3-IN-36
    Inhibitor
    FLT3-IN-36 is a potent FLT3 inhibitor. FLT3-IN-36 exhibits antitumor activity against FLT3-mutated acute myeloid leukemia (AML) cells. FLT3-IN-36 induces cell cycle arrest, reduces mitochondrial membrane potential, and induces apoptosis, downregulating FLT3 and downstream protein expression (including AKT, ERK, PI3K, and STAT5). FLT3-IN-36 can be used for AML research.
    FLT3-IN-36
  • HY-168043
    STAT3-IN-35
    Inhibitor
    STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model.
    STAT3-IN-35
  • HY-159157
    Anti-inflammatory agent 92
    Inhibitor
    Anti-inflammatory agent 92 (compound LD4) is a porphyrin derivative. Anti-inflammatory agent 92 has anti-inflammatory properties. Anti-inflammatory agent 92 can alleviate ulcerative colitis by inhibiting the STAT3-EPHX2 axis.
    Anti-inflammatory agent 92
  • HY-P10854
    TAT-N15
    Inhibitor
    TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke.
    TAT-N15
  • HY-182380
    ODZ10117
    Inhibitor
    ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC50 of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease.
    ODZ10117
  • HY-168903
    STAT3-IN-41
    Inhibitor
    STAT3-IN-41 (Compound 16) is a prodrug of compound 1. STAT3-IN-41 slowly releases compound 1 inhibiting STAT3 signaling pathway. STAT3-IN-41 shows antitumor activity against lung cancer, hepatocellular carcinoma and pancreatic cancer.
    STAT3-IN-41
  • HY-164216A
    (trans)-STAT6-IN-13
    Modulator
    (trans)-STAT6-IN-13 (Compound 95) is a STAT6 inhibitor with IC50 values of ≤300 nM. (trans)-STAT6-IN-13 has weak inhibitory for STAT3. (trans)-STAT6-IN-13 can be used for the researches of cancer, inflammation and immunology.
    (trans)-STAT6-IN-13
  • HY-14743A
    Golotimod TFA
    Inhibitor
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
    Golotimod TFA
  • HY-P992321
    BAY-356
    Activator
    BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer[1][2].
    BAY-356
  • HY-175849
    ALK degrader 1
    Inhibitor
    ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research.
    ALK degrader 1
  • HY-179687
    JAK2-IN-18
    Inhibitor
    JAK2-IN-18 (Compound example1) is a selective JAK2 inhibitor. JAK2-IN-18 can inhibit JAK-STAT signaling and shows an IC50 of <100 nM for pSTAT5 in HEL9217 cells. JAK2-IN-18 can inhibit the proliferation of abnormally proliferating myeloid cells and can be used for the research of myeloproliferative disorders, such as essential thrombocythemia.
    JAK2-IN-18
  • HY-168730
    Anticancer agent 259
    Modulator
    Anticancer agent 259 (Compound 3g) is a Telmisartan (HY-13955)-based cell death modulator, that interfers with the STAT5 signaling pathway, enhances the sensitivity of drug-resistant cells to Imatinib (HY-15463) with SC50 of 1.5 μM.
    Anticancer agent 259
  • HY-N0193S
    Artesunate-d3
    Inhibitor
    Artesunate-d3 is the deuterium labeled Artesunate. Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
    Artesunate-d<sub>3</sub>
  • HY-128450
    JAK-STAT-IN-1
    Inhibitor
    JAK-STAT-IN-1 (compound 1) is a selective JAK-STAT inhibitor. JAK-STAT-IN-1 can be used for the research of autoimmune disorder.
    JAK-STAT-IN-1
  • HY-12352
    HJC0416
    Inhibitor
    HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces Apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity.
    HJC0416
  • HY-165386
    TU-100
    Inhibitor
    TU-100 is a Japanese herbal medicine. TU-100 exhibits anti-cancer effects by regulating cancer-associated fibroblasts (CAFs) in the TME. TU-100 can antagonize the M2 polarization phenotype of macrophages in the tumor microenvironment by suppressing the TLR4/NF-κB/STAT3 axis. TU-100 can inhibit the high expression of MMP-2, COX-2, and VEGF in TAMs.
    TU-100
Cat. No. 상품명 / Synonyms Application Reactivity

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