Interleukin Related Inhibitor

HGR4113 is an orally active anti-inflammatory/antioxidant agent with improved glucose metabolism. HGR4113 inhibits STAT3 phosphorylation, suppresses Th17 differentiation and IL-17 production, reduces oxidative phosphorylation activity, and promotes the differentiation of regulatory T cells among splenic CD4⁺ T cells. HGR4113 inhibits LPS (HY-D1056)-induced JNK phosphorylation, production of NO, PGE₂ and pro-inflammatory cytokines, expression of iNOS and COX-2, as well as nuclear translocation of NF-κB in macrophages, while induces HO-1 expression by activating nuclear translocation of Nrf2. HGR4113 can be used in the research of inflammatory diseases such as type 2 diabetes and Sjögren's syndrome.

CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits T_reg cell development.

Ritlecitinib (PF-06651600) malonate 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 malonate 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 malonate 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).

Methotrexate monohydrate (Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate) is an orally active antifolate (Antifolate). Methotrexate monohydrate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate monohydrate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate monohydrate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate monohydrate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

Talmapimod (SCIO-469) hydrochloride is an orally active and selective inhibitor of p38α MAPK with an IC₅₀ of 9 nM. Talmapimod hydrochloride inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. Talmapimod hydrochloride inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod hydrochloride can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).

MC4762 is an inhibitor of NOX2 and MAOB, with IC₅₀ values of 0.155 μM and 0.182 μM, respectively. MC4762 has anti-inflammatory activity, can inhibit the production of ROS, and downregulate the expression of pro-inflammatory cytokines iNOS, IL-1β, and IL-6.

Seladelpar Lysine dihydrate (MBX-8025 lysine dihydrate) is an orally active, selective PPAR-δ agonist with an EC₅₀ of 2 nM against hPPAR-δ. Seladelpar Lysine dihydrate reduces serum IL-31 and bile acid levels. It alleviates pruritus symptoms. Seladelpar Lysine dihydrate enhances insulin sensitivity, normalizes levels of hyperglycemia, hyperinsulinemia, glucose disposal capacity, serum lipids and hepatic free cholesterol. It reduces steatosis, hepatic inflammation and improves liver fibrosis. Seladelpar Lysine dihydrate reverses the pathological changes of non-alcoholic steatohepatitis (NASH). It is applicable to research related to primary biliary cholangitis and non-alcoholic steatohepatitis (NASH).

PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1. PIPE-791 inhibits LPA-induced calcium mobilization, collagen expression, histamine release, and the activation of fibroblasts, microglia and macrophages. PIPE-791 induces oligodendrocyte precursor cell differentiation, myelination and remyelination, and increases the number of microglia in the retina of normotensive rats. PIPE-791 protects mature oligodendrocytes from cytokine-induced death, reduces the levels of pulmonary fibrosis markers and alleviates neuroinflammation in preclinical models. PIPE-791 can be used in the research of glaucoma, neuroinflammatory diseases, chronic osteoarthritis pain, idiopathic pulmonary fibrosis and multiple sclerosis.

P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC₅₀ value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease.

Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.

Anti-inflammatory agent 99 is a chalcone derivative. Anti-inflammatory agent 99 inhibits LPS (HY-D1056)-induced NF-κB nuclear translocation and suppress the phosphorylation of JNK, ERK, and p38. Anti-inflammatory agent 99 inhibits the expression of cytoinflammatory factors such as TNF-α and IL-6 induced by LPS. Anti-inflammatory agent 99 can be used for the research of LPS-induced septic shock.

AGN-190121 is a selective RARβ/γ retinoid agonist that inhibits IL-6 expression and cell proliferation in cancer cells by antagonizing NF-IL6. AGN-190121 can be used for the research of Kaposi's sarcoma.

DpC hydrochloride is a selective, orally active iron chelator with anticancer activity. DpC hydrochloride acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC hydrochloride induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC hydrochloride inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC hydrochloride is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer.

Selnoflast calcium (RO7486967 calcium), formerly somalix/RG6418/IZD334, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast calcium is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast calcium is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease.

A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC₅₀=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.

Nomelcitinib is a TYK2 inhibitor that modulates the IL23 signaling pathway. Nomelcitinib is used for research on multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease, systemic lupus erythematosus, psoriasis, psoriatic arthritis, Crohn's disease, Sjögren's syndrome, and scleroderma.

Selnoflast potassium (RO7486967 potassium), formerly somalix/RG6418/IZD334, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast potassium is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast potassium is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease.

Diallyl Trisulfide (Standard) is the analytical standard of Diallyl Trisulfide. This product is intended for research and analytical applications. Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer[1][2][3][4].

NLRP3-IN-72 (Compound 2) is a benzimidazole derivative. NLRP3-IN-72 exhibits anti-inflammatory and antioxidant activities. NLRP3-IN-72 has an IC₅₀ of 0.3 μM for NLRP3 IL-1β, a PD₅₀ of 0.4 μM for protecting against pyroptosis, and an EC₅₀ of 0.6 μM for inducing HO-1.

NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an K_D value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release.