inflammation-related diseases

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) exhibits anti-inflammatory, antibacterial, and antifungal activities, along with moderate antitrypanosomal activity, having an MIC value of 19.0 µg/mL.

LTB4-IN-1 (Anti-inflammatory agent 2, Compound 6) belongs to small molecule inhibitors and is a leukotriene B4 (LTB4) synthesis inhibitor (IC50 = 70 nM) with good anti-inflammatory activity. This compound can be used in experimental research on inflammation-related diseases.

MCC950 (CP-456773) is a NLRP3 inflammasome inhibitor (IC50=7.5-8.1 nM). MCC950 can be used to treat inflammatory diseases, inflammation-related tumors and neurodegenerative diseases.

ROCK-IN-1, a potent ROCK inhibitor, effectively inhibits ROCK2-mediated signaling with an IC50 value of 1.2 nM. ROCK-IN-1 is applicable in the study of neurological disorders and inflammation-related diseases.

BMS-561392 Formic acid (BMS-561392 formate) is a small molecule inhibitor, the formate salt form of BMS-561392. As a selective TACE inhibitor and ADAM17 blocker, this compound reduces TNFα levels and is primarily used for research on inflammation-related diseases such as inflammatory bowel disease.

β-Aminoarteether (SM934 free base), an orally active derivative of Artemisinin, serves a pivotal role in the research of inflammation and autoimmune disorders, including those related to lupus diseases.

IRAK4-IN-8 (VI-177) is an IRAK4 inhibitor used to study diseases related to cancer and inflammation.

IRAK inhibitor 2 (IRAK-IN-2) is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK-4) for the study of inflammation-related diseases.

α-Vitamin E is a naturally occurring form of vitamin E with antioxidant and anti-inflammatory activity. α-Vitamin E can be used in research on oxidative stress, lipid peroxidation, membrane damage, and inflammation-related diseases.

Acesulfame inhibits CA9/12 and can be used to study inflammation-related diseases.

1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia/inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

LN-439A is a novel tetrahydro-β-carboline small molecule that acts as a potent catalytic inhibitor of the BAP1 deubiquitinase. It induces ubiquitination and degradation of the KLF5 transcription factor by binding to the catalytic pocket of BAP1. In basal-like breast cancer (BLBC) models, LN-439A significantly inhibits tumor cell proliferation and migration, induces G2/M phase arrest and apoptosis, and exhibits superior water solubility compared to existing BAP1 inhibitors. Furthermore, inhibition of BAP1 enzymatic activity by LN-439A also destabilizes its substrates, suggesting potential application value in inflammation-related diseases.

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

Cyclo(L-Pro-L-Val), a 2,5-diketopiperazine extracted from the fruits of Mycobacterium chiliolyticum AZ2 and Mycobacterium leprae, possesses anti-inflammatory activity and virulence activity against phytopathogenic microorganisms (e.g., R. fascians LMG 3605) and inhibits Gram-positive plant pathogens.Cyclo(L-Pro-L-Val) significantly inhibited IKKα phosphorylation and IκBα and NF-κB activation as well as iNOS and COX-2 activation in a concentration Cyclo(L-Pro-L-Val) significantly inhibited the phosphorylation of IKKα, IKKβ, IκBα, and NF-κB, as well as the activation of iNOS and COX-2 in a concentration-dependent manner, and is a potential therapeutic agent for the treatment of inflammation-related diseases.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G protein-coupled inwardly-rectifying potassium channels (GIRK) through binding to CB1 and CB2 receptors, demonstrating significant cannabinoid-like activity. Its EC50 values are 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be applicable for research in pain management, neurodegenerative diseases, and inflammation-related mechanisms.

PARP1-IN-36 (compound 11) is a derivative of 4-carboxamide-isoindolinone and acts as a selective PARP-1 inhibitor with a Kd value of less than 0.01 μM. This compound is utilized in research related to cancer, cardiovascular diseases, neurological injuries, and inflammation.

EGR-1-IN-3 (Compound 36) is an inhibitor of early growth response 1 (EGR-1) binding to DNA. It effectively suppresses the binding of EGR-1 to DNA and the expression of inflammation-related genes (such as TSLP, IL-31, IL-6, and CCL2) induced by TNFα. This compound is applicable to the study of inflammatory diseases.

PDE4-IN-26 (Compound A5) is an orally active, highly selective inhibitor of PDE4. It exhibits anti-inflammatory properties by inhibiting p38 MAPK phosphorylation. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 reduces lung inflammation, damage, and fibrosis, while promoting sputum secretion and alleviating cough. It is useful for researching lung injury-related diseases.

GSK-3β inhibitor26 (Compound D14) is a GSK-3β inhibitor with an IC50 of 18.23 μM. This compound is applicable in research related to cancer, inflammation, and neurodegenerative diseases.

STING-IN-11 (Compound 42) is a potent, orally bioavailable STING inhibitor (IC₅₀ = 37.8 nM) that blocks STING protein palmitoylation and downstream signaling, thereby inhibiting STING-mediated inflammation.

RIPK2/3-IN-2 (compound 29) is an effective dual inhibitor of RIPK2 and RIPK3 (IC₅₀ = 12 nM/18 nM) capable of inducing necrosis, making it suitable for research into inflammation-related diseases.

STING-IN-13 is a selective STING inhibitor that effectively suppresses downstream signaling of the STING pathway and STING-mediated inflammation. It exhibits low toxicity and is suitable for research related to STING-associated inflammatory and autoimmune diseases.