STAT Inhibitor

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.

Plumericin is an anti-inflammatory, antioxidant, and antibacterial agent. Plumericin reduces Apoptosis, promotes Nrf-2 and inhibits NF-κB and AhR activation, blocks STAT3 signaling. Plumericin inhibits Mycobacterium tuberculosis growth. Plumericin can be used for the research of chronic kidney disease, vascular diseases, inflammatory bowel diseases, peritonitis, and tuberculosis.

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.

ON012380 is a kinase inhibitor with an IC₅₀ of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia.

LC28 is a STAT3 inhibitor with a human STAT3 K_i of 3.92 μM. LC28 targets the DNA-binding domain of STAT3, inhibits STAT3-DNA binding, and suppresses STAT3 signaling. LC28 induces apoptosis and suppresses survival of cisplatin-resistant ovarian cancer cells. LC28 can be used for the research of Cisplatin (HY-17394)-resistant ovarian cancer.

TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma.

(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.

BP-1-108 is a selective inhibitor of STAT5 (K_i=8.3 μM) with anticancer activity. BP-1-108 induces apoptosis of leukemia cells by inhibiting the phosphorylation of STAT5. BP-1-108 can be used in the study of acute myeloid leukemia and prostate cancer.

Itacnosertib hydrochloride (Standard) is the analytical standard of Itacnosertib (hydrochloride) (HY-109179A). This product is intended for research and analytical applications. Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.

Liensinine (Standard) is the analytical standard of Liensinine (HY-N0484). This product is intended for research and analytical applications. Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.

Phaeosphaeride A is a STAT3 inhibitor with an IC₅₀ of 0.61 mM against human STAT3. It exhibits higher selectivity for STAT3 over STAT1 and STAT5. Phaeosphaeride A inhibits the binding of STAT3 to DNA, STAT3-dependent transcriptional activity, as well as IL-6-induced phosphorylation and signaling of STAT3. Phaeosphaeride A activates the JNK, p38, Akt, CREB and STAT5A/B signaling pathways. Phaeosphaeride A induces oxidative stress (ROS), exerts antiproliferative and growth-inhibitory effects in cancer cells, and shows low cytotoxicity toward non-cancerous cells. Phaeosphaeride A is a phytotoxin and a weak animal toxin, with no antimicrobial activity against tested bacteria and fungi. Phaeosphaeride A can be used in research related to conditions such as cervical cancer and multiple myeloma, as well as weed infestations.

Itacnosertib (Standard) is the analytical standard of Itacnosertib (HY-109179). This product is intended for research and analytical applications. Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC₅₀ of 5.90 μM) and the cell viability of p53 expressing A549R (IC₅₀ of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.