STAT3 Inhibitor

ISS610 is a selective Stat3 inhibitor with an IC₅₀ of 42 μM. ISS610 induces Apoptosis. ISS610 can be used in research related to breast cancer and non-small cell lung cancer.

STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC₅₀ value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer.

K882 (Compound 4e) is a Src inhibitor, with K_D of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.

SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC.

STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a K_d of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer.

ROCK2-IN-19, the non-isotopic form of compound 22d, is an orally active and selective ROCK2 inhibitor with an IC₅₀ value of 13 nM. ROCK2-IN-19 selectively inhibits the phosphorylation of STAT3 at tyrosine 705, and suppresses breast cancer metastasis by disrupting the ROCK2-STAT3 signaling axis. ROCK2-IN-19 exhibits anti-metastatic activity in both cancer cells and xenograft models. ROCK2-IN-19 can be used in breast cancer-related research.

HNSS peptide is a chimeric hybrid peptide composed of the neuroprotective peptide S14G-Humanin and the mitochondria-targeted antioxidant peptide SS31. HNSS peptide is readily cleared in vivo and can be combined with nanocarriers to improve its stability. HNSS can be delivered via the FGFR1-targeting nanocarrier FGL-NP (Cit), ameliorating mitochondrial dysfunction, Aβ deposition, tau hyperphosphorylation, and cholinergic neuronal damage, and alleviating memory deficits in Alzheimer's disease mice. HNSS peptide is applicable for Alzheimer's disease-related research.

Hsp110-STAT3 PPI-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 PPI-IN-2 can be used in pulmonary arterial hypertension (PAH) related research.

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

Tofacitinib-¹³C₃,¹⁵N (Tasocitinib-¹³C₃,¹⁵N; CP-690550-¹³C₃,¹⁵N) is the ¹⁵N, ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC₅₀ of 20 nM against PDGFRA, a K_i of 93.3 nM against CA IX, and a K_i of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.

MMP-2/9-IN-2 (Compound 6k) is a MMP-2 and MMP-9 inhibitor, with IC₅₀ values of 29.27 and 24.87 μM respectively. MMP-2/9-IN-2 exhibits good selective toxicity against multiple human hepatoma cell lines. MMP-2/9-IN-2 induces cell cycle arrest and apoptosis, significantly inhibits cell migration and invasion. MMP-2/9-IN-2 inhibits the phosphorylation of the STAT3 signaling pathway. MMP-2/9-IN-2 shows strong anti-tumor activity in a nude mouse xenograft model of HepG2 liver cancer cells.

JAK2-IN-9 is an orally active selective JAK2 inhibitor with a human IC₅₀ of 5 nM. JAK2-IN-9 inhibits JAK2 kinase activity, blocks JAK2 phosphorylation, and suppresses the activation of the downstream JAK2-STAT signaling pathway. JAK2-IN-9 inhibits the phosphorylation of STAT3, STAT5 and AKT in cancer cells. JAK2-IN-9 induces cancer cell apoptosis (apoptosis) and cell cycle arrest. JAK2-IN-9 can be used for the research of myeloproliferative neoplasms.

PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC₅₀ of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma).

Z169667518 is a ligand of IL-6. Z169667518 can inhibit IL-6-induced STAT3 reporter activity with an IC₅₀ of 2.7 µM. Z169667518 can be used in the research of IL-6-related diseases.

PROTAC RET Degrader 2 is a RET degrader with a target IC₅₀ of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (K_d: 60.03 μM) and CAIX (IC₅₀: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).

SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC₅₀ of 30 nM against HDAC1 and an IC₅₀ of 10 nM against HDAC6. SHN7 inhibits STAT3 with a K_d of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.

STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase.

NTZ-24 is a selective STAT3 pathway inhibitor. NTZ-24 suppresses STAT3 phosphorylation at Tyr705, blocks STAT3-DNA interaction, and downregulates the levels of STAT3 downstream target proteins. NTZ-24 induces cell-cycle arrest and promotes apoptosis in cancer cells. NTZ-24 exerts significant antiproliferative activity against HeLa cells (IC₅₀ = 3.3 μM). NTZ-24 can be used for the research of cervical cancer.