ζstat

ζ-Stat (NSC37044), a specific and atypical inhibitor of PKC-ζ with an IC50 of 5 μM, demonstrates the ability to inhibit proliferation and induce apoptosis in melanoma cell lines, exhibiting antitumor activity in vitro[1][2].

ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ) with an IC50 of 5 μM. It effectively suppresses melanoma cell proliferation, induces apoptosis, and shows significant in vitro antitumor activity.

STAT3-IN-B9 (B9) is an inhibitor of abnormal STAT3 activation and inhibits the proliferation of tumor cells including MDA-MB-468, MDA-MB-231, and DU145.

STAT3-IN-1 selective and orally active inhibitor of STAT3(in HT29 and MDA-MB 231 cells, with IC50 values of 1.82 μM and 2.14 μM , respectively), induces tumor apoptosis.

STAT5-IN-2 is an inhibitor of STAT5 with antileukemic effects (EC50s: 9 μM and 5 μM in K562 and KU812 cells, respectively).

STAT3-IN-35 is a STAT3 inhibitor that binds to the SH2 domain. This compound inhibits the phosphorylation of STAT3 and exhibits antiproliferative activity in triple-negative breast cancer (TNBC) cell lines. Additionally, STAT3-IN-35 has demonstrated toxicity and potent antitumor activity in TNBC xenograft models.

STAT3HiBiT degrader 1 is a potent degrader of STAT3HiBiT, exhibiting a DC50 of less than 0.05 μM in A549 cells.

STAT3-IN-36 (compound 11g) is a tritarget inhibitor that selectively targets LRPPRC, STAT3, and CDK1, exhibiting potent anticancer activity. This compound binds to LRPPRC, STAT3, and CDK1, demonstrating more effective anticancer effects than those of TMF or Capecitabine. Additionally, STAT3-IN-36 exhibits an IC50 value of 1.8 μM in HGC27 cells.

STAT3-IN-39 (compound 10K) is an orally active inhibitor of STAT3, demonstrating effective inhibition of STAT3 phosphorylation with an IC50 of 0.47 μM in NIH-3T3 cells. It hinders TGF-β1-induced fibrotic responses and prevents epithelial-mesenchymal transition in A549 cells. STAT3-IN-39 is applicable for research related to idiopathic pulmonary fibrosis.

STAT3-IN-37 (Compound 101) is an inhibitor of STAT3, with an IC50 of 15 nM as measured by DNA-HTRF assay and 2 nM as determined through human whole blood SOCS3 qPCR assay.

STAT1/3-IN-1 (Compound 6k) is an inhibitor of STAT1/3 phosphorylation. It prevents the phosphorylation and nuclear translocation of STAT1/3. Additionally, STAT1/3-IN-1 inhibits the inflammatory enzymes iNOS and COX-2. This compound exhibits anti-inflammatory properties by reducing pro-inflammatory cytokines, such as IL-1β, IL-6, and TNF-α, without significant cytotoxicity.

STAT3-IN-40 (Compound 8b) is an anticancer agent. It initiates immune responses in CD4+ and CD8+ T lymphocytes by inhibiting the expression and phosphorylation of STAT3, and induces ferroptosis and apoptosis in tumor cells. STAT3-IN-40 is valuable for research into cancer chemoimmunotherapy drugs.

STAT3-IN-41 (Compound 16) is a prodrug of compound 1. It gradually releases compound 1, which inhibits the STAT3 signaling pathway. STAT3-IN-41 exhibits antitumor activity against lung cancer, hepatocellular carcinoma, and pancreatic cancer.

STAT5-IN-3 (Compound 14a) is a STAT5 inhibitor with anticancer properties. It works by blocking the tyrosine phosphorylation of STAT5A/5B at the Y694/699 sites, significantly reducing the expression of the STAT5B protein. This leads to the inhibition of downstream gene transcription, thereby preventing the proliferation and survival of leukemia cells. Additionally, STAT5-IN-3 has significant potential in overcoming chemotherapy resistance.

JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

STAT4-IN-1 is a STAT4 inhibitor with a Ki of 0.35 μM. It holds promise for research into autoimmune diseases, including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes.

AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is a modulator of the AKR1B1/STAT3/SLC7A11 pathway, capable of reversing DOX resistance in MCF-7/ADR cells by enhancing ferroptosis (apoptosis) activity. It is utilized in breast cancer research.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). It induces ferroptosis by elevating reactive oxygen species (ROS) and lipid peroxides. This compound also inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 is applicable for research in triple-negative breast cancer (TNBC).

STAT6-IN-7 (Compound 178) is a STAT6 inhibitor with an IC50 of 0.28 μM for inhibiting the binding of human STAT6/pIL-4Rα. It is utilized in research related to inflammation and allergic diseases.

STAT3-IN-43 (Compound K2) is a covalent inhibitor targeting an allosteric site at the interface between the coiled-coil domain and the DNA-binding domain of STAT3, with an IC50 of 40.7 μM. It is applicable in cancer research.

STAT3-IN-46 is a selective, orally active inhibitor of the signal transducer and activator of transcription 3 (STAT3), with a KD value of 323.3 nM. It binds directly to the SH2 domain of STAT3, inhibiting the IL-6/JAK/STAT3 signaling pathway with an IC50 value of 0.87 μM, and decreases levels of c-Myc and Bcl-2. STAT3-IN-46 is applicable in cancer research, including studies on triple-negative breast cancer.

(trans)-STAT6 modulator-5 (Compound 95) is a modulator of the STAT6 protein, inhibiting the STAT6 signaling pathway. This compound holds potential for the research of inflammatory diseases and allergic reactions.

STAT3-IN-47 is an orally active STAT3 inhibitor. It exhibits broad-spectrum antitumor activity against HeLa, HepG2, U87, and LN229 cells. STAT3-IN-47 inhibits STAT3 activation in vitro. This compound is applicable for solid tumor research, particularly in studies of central nervous system (CNS) malignancies and hepatocellular carcinoma.

STAT3-IN-52 (Compound 9) is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3). It binds to the pY705 site of STAT3 with a Ki of 440 nM, effectively hindering STAT3 phosphorylation and dimerization. STAT3-IN-52 exhibits potent cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 of 0.7 μM), medulloblastoma UW426, and pancreatic cancer BKPC3 cells. The compound induces apoptosis, inhibits STAT3's nuclear translocation and DNA-binding activity, and downregulates the expression of the STAT3 target gene MMP9. STAT3-IN-52 is useful in research related to cancers with aberrant STAT3 activation.