STAT Inhibitor

Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis.

Fludarabine (Standard) is the analytical standard of Fludarabine. This product is intended for research and analytical applications. Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.

STX-0119 (Standard) is the analytical standard of STX-0119 (HY-103692). This product is intended for research and analytical applications. STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC₅₀ of 74 μM.

Ritlecitinib (Standard) is the analytical standard of Ritlecitinib (HY-100754). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) 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 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 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).

inS3-54-A26 is a STAT3 inhibitor. inS3-54-A26 has a toxic IC₅₀ of 4.0 μM for non-cancerous lung fibroblasts.

L002 (Standard) is the analytical standard of L002 (HY-100671). This product is intended for research and analytical applications. L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.

Graveoline (Standard) is the analytical standard of Graveoline (HY-12538). This product is intended for research and analytical applications. Graveoline (Rutamine) is an orally active alkaloid with various activities such as antifungal, antiparasitic, anti-inflammatory, and antitumor effects. Graveoline can induce tumor cell apoptosis and autophagy through a reactive oxygen species-mediated pathway. Graveoline has an MIC of 500 μg/mL for Candida albicans. Graveoline can be used in the research of various diseases such as tumors and liver injury.

TPCA-1 (Standard) is the analytical standard of TPCA-1 (HY-10074). This product is intended for research and analytical applications. TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

Homoharringtonine (Standard) is the analytical standard of Homoharringtonine. This product is intended for research and analytical applications. Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

RSVA405 (Standard) is the analytical standard of RSVA405 (HY-103238). This product is intended for research and analytical applications. RSVA405 is a potent, orally active activator of AMPK, with an EC₅₀ of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.

Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

NT157 (Standard) is the analytical standard of NT157 (HY-100037). This product is intended for research and analytical applications. NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway.

(E/Z)-AG490 (Standard) is the analytical standard of (E/Z)-AG490 (HY-107459). This product is intended for research and analytical applications. (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

2,4,5-Trimethoxybenzoic acid (Standard) is the analytical standard of 2,4,5-Trimethoxybenzoic acid (HY-Y0586). This product is intended for research and analytical applications. 2,4,5-Trimethoxybenzoic acid (Asaronic acid) is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits LPS (HY-D1056)-induced inflammatory responses, inhibits the activation of NF-κB and STAT signaling pathways. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes.

STAT5-IN-2 (Standard) is the analytical standard of STAT5-IN-2 (HY-102048). This product is intended for research and analytical applications. STAT5-IN-2 is a STAT5 inhibitor, extracted from reference 1, example 17f. STAT5-IN-2 has potent antileukemic effect.

Lorpucitinib (Standard) is the analytical standard of Lorpucitinib (HY-109182). This product is intended for research and analytical applications. Lorpucitinib (JNJ-64251330) is an orally active pan-JAK inhibitor. Lorpucitinib inhibits all four human JAKs, with greatest potency toward JAK1/JAK3 and JAK1/TYK2 heterodimers, and reduces STAT-3 phosphorylation downstream of JAK signaling. Lorpucitinib can be used for the research of gastrointestinal inflammatory diseases.

STAT3-IN-50 (compound HY041004) is a potent STAT3 inhibitor with an IC₅₀ of 0.259 μM. STAT3-IN-50 induces apoptosis and inhibits colon and liver cancer cell proliferation. STAT3-IN-50 can be used for colon and liver cancer research.

Bromisoval (Standard) is the analytical standard of Bromisoval. This product is intended for research and analytical applications. Bromisoval has anti-inflammatory effects.

Golotimod (Standard) is the analytical standard of Golotimod. This product is intended for research and analytical applications. Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).