Interleukin Related Inhibitor

cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM.

PTD-N5-1 is an IRF5 inhibitory peptide. PTD-N5-1 blocks the activation of IRF5. PTD-N5-1 inhibits β-glucan-induced IL-12 production in bone marrow-derived dendritic cells pre-stimulated with IFN-γ. PTD-N5-1 reduces the levels of IL-12 and IFN-γ in the kidneys of mice with Candida albicans infection. PTD-N5-1 is applicable to the research of Candida albicans infection.

Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC₅₀ of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease.

IL-17-IN-2 (Example 51) is a potent inhibitor of IL-17, with the IC₅₀ of < 0.4 μM in HTRF and NHK assay.

Revbekitug is a humanized IgG1κ antibody targeting IL-5. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).

Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC₅₀ values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1 effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI).

Gluconate (D-Gluconic acid) (Standard) is the analytical standard of Gluconate sodium (HY-B1092A). This product is intended for research and analytical applications. Gluconate (D-Gluconic acid) sodium is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.

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

Oturkibart is a humanized immunoglobulin G4-κ monoclonal antibody targeting the human interleukin 4 receptor (IL4R). Oturkibart is promising for research of inflammatory diseases, such as asthma and atopic dermatitis.

CJM112 is a fully human IgG1/κ monoclonal antibody inhibitor targeting IL-17A, which binds to IL-17A and the IL-17AF heterodimer with high affinity, with K_D values of 5.7 pM and <11 pM, respectively. CJM-112 exerts anti-inflammatory effects by neutralizing IL-17A, and reduces the Psoriasis Area and Severity Index in a time- and dose-dependent manner. CJM-112 also exhibits anti-inflammatory activity and improves disease severity in studies of hidradenitis suppurativa. CJM-112 shows favorable biosafety and tolerability. CJM-112 can be used in studies related to psoriasis and hidradenitis suppurativa.

SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC₅₀ of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research of acute hepatitis.

HY-P990973 is an IL17A-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

Methotrexate-d₃ diammonium is the deuterated-labeled Methotrexate (HY-14519). Methotrexate (Amethopterin; CL14377; WR19039) is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate 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.

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC₅₀ of 182 nM.

BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC₅₀ of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research.

1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes.

Anti-Rat IL-4 Antibody (OX-81) is an antibody inhibitor against rat IL-4. Anti-Rat IL-4 Antibody (OX-81) can specifically block the anti-inflammatory effect of IL-4. Anti-Rat IL-4 Antibody (OX-81) can be used for research on inflammation conditions such as experimental allergic encephalomyelitis (EAE).

Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC₅₀ = 0.35 mg/mL), LOX (IC₅₀ = 0.56 mg/mL) and HYAL (IC₅₀ = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).

Acetyl hexapeptide-49 (example 13) is a bioactive peptide with anti-allergen effect and has been reported used as a cosmetic ingredient. Acetyl hexapeptide-49 can alleviate stimulation of mammalian skin cells and protect cell vitality.

Solaprubart (STAR-0310) is a fully human IgG1 subtype monoclonal antibody targeting OX40 (CD134/TNFRSF4), with a K_d of 7.2 nM. By blocking the OX40/OX40L co-stimulatory signal, Solaprubart effectively inhibits cytokine release (IFN-γ, TNF-α, IL-5, IL-13) from activated effector T cells (Th1/Th2/Th17-associated). Solaprubart can be used in research related to moderate-to-severe atopic dermatitis.