STAT Inhibitor

Niclosamide-d₃ (BAY2353-d₃) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC₅₀ of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells.

STAT3-IN-1 (Standard) is the analytical standard of STAT3-IN-1 (HY-100753). This product is intended for research and analytical applications. STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.

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.

Iridin (Standard) is the analytical standard of Iridin. This product is intended for research and analytical applications. Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.

YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth.

XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability.

Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML).

AS1517499 (Standard) is the analytical standard of AS1517499 (HY-100614). This product is intended for research and analytical applications. AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC50 of 21 nM.

HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice.

CT 2576 is a phospholipid signaling inhibitor as well as a Jak3/STAT5 inhibitor. CT 2576 suppresses gene expression and replication of human immunodeficiency virus (HIV) at the post-transcriptional level by interfering with phospholipid metabolism in host cells, particularly by inhibiting the production of phosphatidic acid PA. CT-2576 completely inhibits the growth and proliferation of malignant T-cell lymphoma cells by suppressing phospholipid signaling and blocking the Jak/STAT signaling pathway associated with IL-2R. CT 2576 can be used in research related to human immunodeficiency virus (HIV) infection and cutaneous T-cell lymphoma (CTCL).

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC₅₀ of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1^SER727 with an IC₅₀ of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC₅₀ of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.

Anthraquinone-2-carboxylic acid (Standard) is the analytical standard of Anthraquinone-2-carboxylic acid (HY-W031757). This product is intended for research and analytical applications. Anthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n

Hispidin (Standard) is the analytical standard of Hispidin. This product is intended for research and analytical applications. Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1][2][3][4][5][6][7].

GYY4137 (Standard) is the analytical standard of GYY4137 (HY-107632). This product is intended for research and analytical applications. GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocK_ing the STAT3 pathway, demonstrating potent anticancer activity.

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.

Gliquidone (Standard) is the analytical standard of Gliquidone. This product is intended for research and analytical applications. Gliquidone can bind to the pancreatic β-cells and increases insulin release to regulate blood glucose levels. Gliquidone significantly decreases LPS (HY-D1056)-induced proinflammatory responses and inhibits ERK/STAT3/NF-κB phosphorylation in BV2 microglial cells. Gliquidone can suppress microgliosis, microglial hypertrophy mediated by LPS, and proinflammatory cytokine COX-2 and IL-6 levels in murine model. Gliquidone also exhibits good anticancer activity in lung carcinoma cells. Gliquidone has antioxidant property. Gliquidone can be studied in research for type 2 diabetes and cancers.

DZ2002 (Standard) is the analytical standard of DZ2002. This product is intended for research and analytical applications. DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

BP-1-102 (Standard) is the analytical standard of BP-1-102 (HY-100493). This product is intended for research and analytical applications. BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

Cilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

STAT6-IN-14 is a STAT6 inhibitor that blocks the binding of STAT6-pIL-4Rα, with an IC₅₀ of 1.20 μM. STAT6-IN-14 can inhibit IL-4-induced STAT6 transcriptional activity in STAT6-HEK293 cells. STAT6-IN-14 can be used for research on allergic diseases and inflammation.