STAT3 Inhibitor

STAT4-IN-1 is an inhibitor of STAT4 with a K_i of 0.35 μM. STAT4-IN-1 is expected to be used in the research of autoimmune diseases, including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes.

Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity. Nifuroxazide is an orally active nitrofuran antibiotic.

Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity.

MS4078 is a ALK PROTAC degrader with a DC₅₀ of 11 nM in SU-DHL-1 cells and a DC₅₀ of 59 nM in NCI-H2228 cells, and its K_d value for ALK binding is 19 nM. MS4078 induces ALK degradation via the ubiquitin-proteasome pathway by recruiting cereblon, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4078 is applicable for the research of non-small cell lung cancer and anaplastic large cell non-Hodgkin's lymphoma.

Sarilumab is a monoclonal antibody targeting IL6 that binds to IL6R and blocks the binding of IL6, thereby inhibiting the activation of the downstream STAT3 phosphorylation signaling pathway. In tumor cells with active IL6/STAT3 signaling pathways, Sarilumab induces Apoptosis and inhibits cell growth. Sarilumab is applicable to research related to prostate cancer, lung cancer and rheumatoid arthritis.

STAT1/3-IN-1 is a potent STAT1/3 inhibitor with potent anti-inflammatory effect. STAT1/3-IN-1 inhibits phosphorylation and nuclear translocation of STAT1/3 to modulate microglial inflammation, reduces LPS (HY-D1056)-induced pro-inflammatory cytokines (NO, IL-1β, IL-6, and TNF-α) and inflammatory mediators (iNOS, COX-2). STAT1/3-IN-1 exhibits low toxicity in mice. STAT1/3-IN-1 can be used for the research of neuroinflammation.

Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC₅₀=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.

15-keto-Prostaglandin E2 (15-keto-PGE2) is an endogenous PGE₂ metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to the Cys259 residue of STAT3. 15-keto-Prostaglandin E2 binds to and stabilizes EP2 and EP4 receptors. 15-keto-Prostaglandin E2 inhibits the growth and progression of breast cancer cells. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth. 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development and reduces the surface area of the glomerular filtration barrier.

Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites.

Olokizumab (CDP 6038) is a humanized monoclonal antibody that targets interleukin-6 (IL-6). Olokizumab inhibits IL-6-induced STAT-3 phosphorylation. Olokizumab is used in the study of arthritis.

LLL12 is a small molecule inhibitor of STAT3 that inhibits STAT3 phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth.

STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC₅₀ of 74 μM.

STAT3-IN-25 (Compound 2p) is a potent STAT3 inhibitor with a p-trifluoroethoxy benzyl substituent. STAT3-IN-25 shows STAT3 luciferase inhibition activity using HEK293T cells with an IC₅₀ of 22.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC₅₀ of 32.5 nM. STAT3-IN-25 has the potential for pancreatic cancer research.

HJC0152 is a signal transducers and activators of transcription 3 (STAT3) inhibitor.

Anti-Mouse CD276/B7-H3 Antibody (MJ18) is a rat-derived anti-mouse CD276/B7-H3 IgG1 monoclonal antibody. Anti-Mouse CD276/B7-H3 Antibody (MJ18) can inhibit CD276/B7-H3 and induce tumor cell apoptosis. Anti-Mouse CD276/B7-H3 Antibody (MJ18) enhances anti-tumor immune response by reducing immunosuppressive cells and promoting T cell activation. Anti-Mouse CD276/B7-H3 Antibody (MJ18) can be used for research on cancer such as breast cancer and prostate cancer.

CAY10594 is an orally active PLD2 inhibitor with an IC₅₀ of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.

JMS-053 is an efficient and reversible PTP4A3 inhibitor, with an IC₅₀ value of 18 nM. JMS-053 demonstrates broad PTP4A inhibitory activity with IC₅₀s of 50 nM and 53 nM for PTP4A1 and PTP4A2, respectively. JMS-053 exhibits IC₅₀ values of 92.6 nM and 207.6 nM for CDC25B and DUSP3, respectively. JMS-053 can effectively inhibit the activity of PTP4A3, inhibit tumor cell proliferation and migration through multiple mechanisms such as interfering with RhoA and STAT3/p38 signaling pathway. JMS-053 can be used for the study of cancers such as ovarian cancer, breast cancer and colon cancer.

HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.