stat3 in 3

STAT3-IN-3 is a potent and highly selective targeted STAT3 inhibitor with significant anti-proliferative activity. It effectively induces apoptosis in breast cancer cells. As a mitochondrially targeted STAT3 inhibitor with great research potential, it has good application value in tumor mechanism exploration and anti-cancer research.

JAK2/STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

(R)-JAK2/STAT3-IN-10a is the R-isomer of JAK2/STAT3-IN-1.JAK2/STAT3-IN-1 is a GP130 D1 structural domain inhibitor with antitumor activity that inhibits the phosphorylation of JAK2 and STAT3. The KD value of (R)-JAK2/STAT3-IN-1 on GP130 protein is 3.8 μM.

STAT3/AKT-IN-1 is a dual inhibitor of the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signaling pathways, demonstrating anti-tumor activity and inducing apoptosis in SGC-7901 cells.

STAT3/NF-κB-IN-1 is a potent inhibitor of STAT3 and NF-κB, exhibiting IC50 values of 5.86 μM for STAT3 and 4.22 μM for NF-κB in 4 T1 cells. It induces apoptosis by upregulating key apoptotic regulators (caspases-3, 9, Bax) and downregulating Bcl-2 expression. STAT3/NF-κB-IN-1 shows significant anticancer activity against breast cancer cell lines and can reduce tumor volume in vivo. It is applicable for research in breast cancer.

STAT3/HDAC-IN-2 (compound 18), a dual inhibitor of STAT3 and HDAC, promotes autophagy and apoptosis. This compound features an amphiphilic hydroxamic acid hybrid structure, derived from the natural product isopropanol lactone (IAL), and functions as a nanoscale anticancer agent. It has the ability to self-assemble into nanoparticles in aqueous environments, leading to enhanced tumor tissue accumulation, increased cellular uptake, and improved anticancer efficacy compared to its free state.

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

STAT3ligand 5 is a STAT3 ligand, serving as a target protein ligand for the synthesis of the PROTAC degrader [SD-436].

PROTACSTAT3 degrader-3 (S3D1) is a STAT3 PROTAC degrader with anti-cancer properties.

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).

STAT3-IN-11 is a selective STAT3 inhibitor with inhibitory effects on phosphorylation of the STAT3pTyr705 site and phosphorylation of Survivin.STAT3-IN-11 promotes apoptosis in cancer cells and is a candidate compound for the treatment of cancer.

STAT3-IN-13 is a potent STAT3 inhibitor.STAT3-IN-13 has antiproliferative and anticancer activity and acts by binding to the structural domain of STAT3 SH2.STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705, which induces apoptosis and inhibits tumor cell growth and metastasis.STAT3-IN-13 can be used to study breast cancer and liver cancer. The study of breast cancer and hepatocellular carcinoma.

STAT3 Degrader-1 (Compound 295) is a potent degrader of STAT3, utilized in anticancer research [1].

PROTAC STAT3 degrader-2 is a selective and effective PROTAC degrader of the STAT3 protein, exhibiting a DC50 of 3.54 μM in Molm-16 cells. It holds potential for cancer research [1].

Anti-STAT3 Antibody is an antibody targeting STAT3. It can be used for oncology, signaling pathway, and disease mechanism research.

APT STAT3 is a STAT3-binding peptide that displays high specificity and affinity for STAT3 (～231 nmol/L). It serves as a tractable agent for targeting a wide range of cancers with constitutively activated STAT3 [1].

APTSTAT3, scrambled (APTscr) is a control peptide for the STAT3-specific peptide (APTSTAT3) and does not bind STAT3. APTSTAT3, scrambled retains the same trpzip scaffold, but features a disordered sequence at the target binding site.

STAT3-IN-31 (compound K2071), derived from STATtic, acts as an inhibitor of both STAT3 and mitotic processes. This compound interrupts mitotic progression and impacts the formation of the mitotic spindle. Additionally, STAT3-IN-31 hampers migration in glioblastoma cells, suppresses cellular proliferation within tumor spheroids, induces senescence in glioblastoma, and inhibits the growth of Temozolomide-resistant cells while reducing the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein (MCP-1).

STAT3-IN-34 (Compound 15E) acts as a STAT3 inhibitor, blocking both the nuclear translocation and the transcriptional regulator activity of STAT3. It effectively inhibits HaCaT cell proliferation with an IC50 value of 0.008 μM. Additionally, STAT3-IN-34 reduces IL-17A expression and mitigates Imiquimod-induced psoriasis in mouse models.

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.

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-38 (Compound 4m) is a STAT3 inhibitor with a dissociation constant (K_D) of 45.33 µM for rhSTAT3, and is a derivative of Celastrol. It binds to the SH2 domain of the STAT3 protein, inhibiting phosphorylation at the pTyr705 site and suppressing downstream gene expression of Survivin and Mcl-1. STAT3-IN-38 can arrest the cell cycle and induce apoptosis in colorectal cancer cells.