STAT3 Inhibitor

Balsalazide disodium is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway.

Cyclo (L-Ile-D-Leu) (Compound 15) is a STAT3 inhibitor. Cyclo (L-Ile-D-Leu) is isolated from the culture broth of Lactococcus lactis KR-050L. Cyclo (L-Ile-D-Leu) inhibits IL-6-induced STAT3 activation in cancer cells. Cyclo (L-Ile-D-Leu) is applicable to hepatocellular carcinoma research.

15-Keto-prostaglandin E2-d₄ is the d₄ labeled 15-keto-Prostaglandin E2 (HY-113205). 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.

Tofacitinib-¹³C (Tasocitinib-¹³C; CP-690550-¹³C) is the 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.

GYY4137 (GMP) is the GMP-grade version of GYY4137 (HY-107632). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. GYY4137 (GMP) is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GYY4137 (GMP) can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.

Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride 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 hydrochloride 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 hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

TT-301 hydrochloride is a small-molecule immunomodulator capable of penetrating the blood-brain barrier. TT-301 hydrochloride exerts neuroprotective effects by binding to IL-1β, downregulating STAT3 expression, and modulating the JAK-STAT signaling pathway, thereby inhibiting microglial activation and the release of proinflammatory mediators, and alleviating neuroinflammation and brain edema. TT-301 hydrochloride is used in research on traumatic brain injury, intracerebral hemorrhage, subarachnoid hemorrhage, muscle wasting and atrophy, and periodontal disease.

DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC₅₀ values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy.

Isocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma^[1][2].

STAT3-IN-39 (compound 10K) is an orally active STAT3 inhibitor that exhibits excellent inhibitory activity against STAT3 phosphorylation, with an IC₅₀ of 0.47 μM in NIH-3T3 cells. STAT3-IN-39 inhibits the TGF-β1-induced fibrotic response and blocks the epithelial-mesenchymal transition in A549. STAT3-IN-39 can be utilized in research related to idiopathic pulmonary fibrosis.

Pulchinenoside E2 is a triterpenoid saponin. Pulchinenoside E2 inhibits the phosphorylation of STAT3 and JAK2, blocks the nuclear translocation and transcriptional activity of STAT3, and suppresses STAT3-dependent mitochondrial oxidative phosphorylation. Pulchinenoside E2 inhibits invasion, migration and autophagy of triple-negative breast cancer cells. Pulchinenoside E2 can be used in research related to triple-negative breast cancer.

Tyk2-IN-25 is a TYK2 inhibitor that binds to the JH2 domain of TYK2. Tyk2-IN-25 inhibits p-STAT4 and p-STAT3 in human peripheral blood mononuclear cells. Tyk2-IN-25 is applicable to research related to multiple diseases such as immune and inflammatory diseases, and neurological diseases.

STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

FLLL12 (GO-Y026) is a curcumin analog anticancer agent. FLLL12 inhibits the phosphorylation of AKT, Bcl-2, Bid, EGFR, mTOR, FOXO1a, FOXO3a, STAT3, HER2/neu, as well as pancreatic AKT/STAT3; upregulates the expression of Bim and DR5; and activates PTPs. FLLL12 regulates downstream pathways, induces mitochondria-mediated and DR5-dependent extrinsic apoptosis, inhibits cancer cell viability, proliferation, anchorage-independent growth and migration, and exerts a synergistic effect with Doxorubicin (HY-15142A). FLLL12 can be used in research related to head and neck squamous cell carcinoma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, colon cancer and colorectal cancer.

BXL0124 is an orally effective CD44 inhibitor and Notch signaling pathway inhibitor. BXL0124 has a vitamin D receptor-dependent mechanism and can downregulate the expression of CD44, Notch1/2/3, HES1, OCT4, LAMA5, JAG1, JAG2, NF-κB and DLL1. BXL0124 inhibits c-Myc expression and the levels of phosphorylated ERK, AKT, ErbB2, reduces the level of activated Notch1 receptor and its nuclear localization, decreases the mRNA and protein levels of Jagged-1 and Jagged-2, and inhibits the STAT3 signaling pathway by reducing the formation of the CD44-STAT3-JAK2 complex, while also inhibiting the transcriptional activity of the CD44 promoter in a p53-dependent manner. BXL0124 can induce myoepithelial differentiation and inhibit the self-renewal of cancer stem cell-like cells, cancer cell proliferation, invasion, and growth. BXL0124 can be used in research related to triple-negative breast cancer, basal-like breast cancer, ErbB2-overexpressing mammary tumorigenesis, and breast cancer.

Tofacitinib-d₃ (Tasocitinib-d₃; CP-690550-d₃) is the deuterated-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.

GPA512 is an orally active STAT3 inhibitor and a prodrug of Galiellalactone (HY-125170). GPA512 inhibits the binding of STAT3 to DNA, downregulates STAT3-activated genes, and suppresses tumor growth in prostate cancer xenograft models. GPA512 is rapidly converted to Galiellalactone in plasma. GPA512 can be used in research related to castration-resistant prostate cancer.

Madindoline A is an orally active gp130 antagonist with a K_D of 288 μM. Madindoline A inhibits IL-6- and IL-11-induced osteoclastogenesis, suppresses IL-6-stimulated serum amyloid A protein production, inhibits bone resorption and bone loss, and also inhibits IL-6- and IL-11-dependent cell line growth, as well as IL-6-dependent Stat3 tyrosine phosphorylation. Madindoline A is applicable for the research of hormone-dependent postmenopausal osteoporosis.

Betavulgarin is an anticancer agent. Betavulgarin can be isolated from Sugar Beet (Beta vulgaris). Betavulgarin suppresses the proliferation, migration, colony formation, and mammosphere formation of breast cancer cells, and reduces the size of the CD44⁺/CD24⁻ subpopulation and the expression of the self-renewal- related genes C-Myc, Nanog and Oct4. Betavulgarin promotes BCSCs death through the regulation of Stat3/Sox2 signaling.