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-111275
    WP-1034
    		Inhibitor
    WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.
    WP-1034
  • HY-138071
    8α-Tigloyloxyhirsutinolide 13-O-acetate
    		Inhibitor
    8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.
    8α-Tigloyloxyhirsutinolide 13-O-acetate
  • HY-N6940R
    Prosapogenin A (Standard)
    		Inhibitor
    Prosapogenin A (Standard) is the analytical standard of Prosapogenin A. This product is intended for research and analytical applications. Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
    Prosapogenin A (Standard)
  • HY-107592
    ACHP
    		Inhibitor
    ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies.
    ACHP
  • HY-N0201R
    Atractylenolide I (Standard)
    Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. 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 (Standard)
  • HY-122759
    CPA-7
    		Inhibitor
    CPA7 is a novel Stat3 inhibitor. CPA7 downregulates survivin, Bcl-XL, and Mcl-1. CPA7 induces Apoptosis. CPA7 enhances the radiosensitivity of prostate cancer. CPA7 has anti-cancer effects against prostate cancer.
    CPA-7
  • HY-N16465
    Cinnamtannin D1
    		Inhibitor
    Cinnamtannin D1 is an orally active polyphenolic compound with immunosuppressive activity. Cinnamtannin D1 regulates the balance of Th17/Treg cells by inhibiting AHR expression. Cinnamtannin D1 reduces apoptosis and ROS in INS-1 cells and primary cultured murine islets induced by Palmitic acid (PA) (HY-N0830). Cinnamtannin D1 reduces Th17 cell differentiation via downregulating p-STAT3/RORγt and promotes Treg cell differentiation via upregulating p-STAT5/Foxp3. Cinnamtannin D1 exerts excellent anti-arthritic efficacy in collagen-induced arthritis (CIA) model of mice. Cinnamtannin D1 can be used for the study of rheumatoid arthritis (RA).
    Cinnamtannin D1
  • HY-176535
    KB-0118
    		Inhibitor
    KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
    KB-0118
  • HY-N0701R
    (-)-Asarinin (Standard)
    		Inhibitor
    (-)-Asarinin (Standard) is the analytical standard of (-)-Asarinin (HY-N0701). This product is intended for research and analytical applications. (-)-Asarinin is a tetrahydrofurofurano lignan with various biological activities. (-)-Asarinin induces apoptosis in cancer cells. (-)-Asarinin promotes mitochondrial ROS accumulation, inhibits the STAT3 signaling pathway and induces apoptosis in precancerous cells. (-)-Asarinin is a Src family kinase inhibitor that suppresses mast cell activation. (-)-Asarinin is a non-competitive Δ5-desaturase inhibitor with a Ki of 0.28 mM. (-)-Asarinin possesses pain relief, anti-viral, anti-allergic and anti-tuberculous bacilli, and anti-tumor effects.
    (-)-Asarinin (Standard)
  • HY-171656
    G721-0282
    		Inhibitor
    G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
    G721-0282
  • HY-170946
    WR-S-462
    		Inhibitor
    WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis.
    WR-S-462
  • HY-178936
    JAK2-IN-15
    		Inhibitor
    JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (HY-114134) (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV).
    JAK2-IN-15
  • HY-124067
    EC-70124
    		Inhibitor
    EC-70124 is an orally active multikinase inhibitor targeting IKKβ and JAK2. EC-70124 blocks IkB phosphorylation and STAT3 (Tyr705) activation, suppressing NF-κB nuclear translocation and STAT3 transcriptional activity. EC-70124 reduces tumor growth and cancer stem cell (CSC) populations in prostate cancer cells and xenograft models. EC-70124 is promising for research of prostate cancer.
    EC-70124
  • HY-N0174R
    Cryptotanshinone (Standard)
    		Inhibitor
    Cryptotanshinone (Standard) is the analytical standard of Cryptotanshinone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-170977
    JAK1/STAT3-IN-1
    		Inhibitor
    JAK1/STAT3-IN-1 (compound 4f) is an anti-AD (atopic dermatitis) agent by inhibiting JAK1/STAT3 signaling pathway. JAK1/STAT3-IN-1 inhibits NO generation with an IC50 of 2.17 μM. JAK1/STAT3-IN-1 improves the skin condition of AD-like mice, reduces inflammatory infiltration, inhibits the expressions of p-JAK1/JAK1 and p-STAT3/STAT3, and mitigates the excessive immune response on Calcipotriol (HY-10001) (MC903)-induced AD-like mice.
    JAK1/STAT3-IN-1
  • HY-170576
    FLT3-IN-28
    FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD.
    FLT3-IN-28
  • HY-170927
    JAK-IN-40
    		Inhibitor
    JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC50s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI50 of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772).
    JAK-IN-40
  • HY-168954
    CSF1R-IN-26
    		Inhibitor
    CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22%.
    CSF1R-IN-26
  • HY-P10101
    APT STAT3, scrambled
    		Control
    APT STAT3, scrambled (APTscr), a control peptide of STAT3-specific aptide (APTSTAT3), does not bind STAT3. APT STAT3, scrambled contains the same trpzip scaffold but with a scrambled sequence in the target-binding site.
    APT STAT3, scrambled
  • HY-175781
    CHI3L1-IN-4
    		Inhibitor
    CHI3L1-IN-4 (Compound 8) is a Chitinase-3-Like Protein 1 (CHI3L1) inhibitor with a Kd of 6.8  μM. CHI3L1-IN-4 significantly reduces glioblastoma (GBM) spheroids viability and attenuates phospho-STAT3 levels by disrupting CHI3L1 pathway. CHI3L1-IN-4 can be used for GBM research.
    CHI3L1-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
STAT Isoform Comparison

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