STAT Inhibitor

AG490 (Standard) is the analytical standard of AG490 (HY-12000). This product is intended for research and analytical applications. AG490 (Tyrphostin AG490) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Corylifol A (Standard) is the analytical standard of Corylifol A. This product is intended for research and analytical applications. Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC₅₀ of 0.81 μM.

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.

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.

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.

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.

Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.

Ritlecitinib (tosylate) (Standard) is the analytical standard of Ritlecitinib (tosylate) (HY-100754C). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects.

C188-9 (Standard) is the analytical standard of C188-9 (HY-112288). This product is intended for research and analytical applications. C188-9 (TTI-101) is a STAT3 inhibitor with a K_d value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.

(R)-Lisofylline (Standard) is the analytical standard of (R)-Lisofylline (HY-109854A). This product is intended for research and analytical applications. (R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC₅₀ of 0.6 μM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.