STAT Inhibitor

Corylin (Standard) is the analytical standard of Corylin. This product is intended for research and analytical applications. Corylin is an orally active flavonoid anti-inflammatory and osteogenic agent that inhibits IL-6-induced STAT3 promoter activity and STAT3 phosphorylation. Corylin also has anticancer, antiatherosclerotic, and ameliorating activity in hyperlipidemia and insulin resistance, inducing adipocyte browning and lipolysis through SIRT1 or β3-AR-dependent pathways.

JAK2-IN-14 is an orally active JAK2 inhibitor with an IC₅₀ of 2 nM. JAK2-IN-14 demonstrates 89.5-, 80.5-, and 51-fold selectivity over JAK1, JAK3, and TYK2, respectively. JAK2-IN-14 inhibits STAT5 signaling pathway. JAK2-IN-14 causes tumor cell cycle arrest and apoptosis. JAK2-IN-14 can used for the study of myeloproliferative neoplasms (MPNs).

Cyanidin 3,5-diglucoside (chloride) (Standard) is the analytical standard of Cyanidin 3,5-diglucoside (chloride) (HY-129138). This product is intended for research and analytical applications. Cyanidin 3,5-diglucoside chloride is an anthocyanin. Cyanidin 3,5-diglucoside chloride inhibits inflammatory cytokines (IL-1α, IL-1β, and IL-6) expression and NO production. Cyanidin 3,5-diglucoside chloride inhibits the phosphorylation of STAT3, IκB, ERK, p38, and AKT. Cyanidin 3,5-diglucoside chloride inhibits high pressure-induced decrease in GLAST. Cyanidin 3,5-diglucoside chloride exerts anti-inflammatory and skin barrier modulating effects. Cyanidin 3,5-diglucoside chloride can be used in retinal research.

Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells.

STAT6-IN-13 (Compound 22) is a STAT6 inhibitor with IC₅₀ values of ≤300 nM. STAT6-IN-13 has weak inhibitory for STAT3. STAT6-IN-13 can be used for the researches of cancer, inflammation and immunology.

Gondoic acid (Standard) is an analytical standard for Gondoic acid. This product is used for research and analytical applications. Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts. Gondoic acid can exert anti-inflammatory activity by inhibiting the production of ROS and the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid can be used as a raw material for medical supplies and a moisturizing ingredient in cosmetic creams.

(Rac)-8-Gingerol is a non-volatile component. (Rac)-8-Gingerol can be extracted from ginger. (Rac)-8-Gingerol enhances Apoptosis. (Rac)-8-Gingerol decreases the level of phosphorylated EGFR and, accordingly, the phosphorylation levels of its downstream effectors, STAT3 and ERK. (Rac)-8-Gingerol exhibits anticancer activity against colorectal cancer.

TT-301 is a small-molecule immunomodulator capable of penetrating the blood-brain barrier. TT-301 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 is used in research on traumatic brain injury, intracerebral hemorrhage, subarachnoid hemorrhage, muscle wasting and atrophy, and periodontal disease.

Kansuinine B is a natural diterpenoid compound with anti-inflammatory, anti-cancer and anti-viral activities, which can be isolated from the roots of Euphorbia kansui. Kansuinine B induces sustained ERK1/2 activation, inhibits IL-6-induced Stat3 activation and tyrosine phosphorylation, and enhances serine phosphorylation of Stat3. Kansuinine B negatively regulates the IL-6 signaling pathway by upregulating the expression of SOCS-3. Kansuinine B promotes the proliferation of mouse splenic lymphocytes in vitro and stimulates rat peritoneal macrophages to produce NO. Kansuinine B can be used in studies related to liver cancer and COVID-19.

ISS840 is a selective STAT1 inhibitor, with an IC₅₀ of 31 μM against STAT1 and an IC₅₀ of 560 μM against STAT3. ISS840 is applicable for cancer research.

Ochromycinone (Standard) ((Rac)-STA-21 (Standard)) is the analytical standard of Ochromycinone (HY-18061). This product is intended for research and analytical applications. Ochromycinone is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.

CHI3L1-IN-6 (Compound 9e) is a CHI3L1 inhibitor with a K_d of 19.11 μM for hCHI3L1. CHI3L1-IN-6 blocks CHI3L1-Galectin-3 interaction. CHI3L1-IN-6 reduces STAT3 signaling. CHI3L1-IN-6 exhibits anti-cancer activity against glioblastoma.

Nifuroxazide-¹³C₆ is the ¹³C₆ labeled Nifuroxazide. Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.

FLC-8 is an orally active FLT3 inhibitor with IC₅₀ values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia.

Bufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3^tyr705, p-Stat3^ser727 and Jak2 expressions. Bufothionine upregulates Atg5, Atg7 and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer.

INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma.

Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model.

ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a K_d of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC).

HZ-1127 is a thymic stromal lymphopoietin (TSLP) inhibitor. HZ-1127 selectively binds to TSLP, blocks receptor complex interaction, inhibits STAT5 activation, downstream inflammatory signaling, and TSLP-induced CCL17 and CCL22 secretion. HZ-1127 can be used for the research of allergic diseases and cancer.

EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research.