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.

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.

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.

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.

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.

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.

TLR4/JNK/NF-κB-IN-1 (Racemic-11k) is an inhibitor of TLR4, JNK, and NF-κB. It suppresses NO production in LPS-stimulated RAW264.7 cells with an IC50 of 23.2 µM. By inhibiting TLR4 expression and reducing JNK phosphorylation, TLR4/JNK/NF-κB-IN-1 prevents NF-κB activation. This leads to a decrease in the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and the production of inflammatory mediators such as NO, PGE2, and TNF-α, thereby exhibiting anti-inflammatory activity. TLR4/JNK/NF-κB-IN-1 holds potential in the study of inflammatory diseases, including rheumatoid arthritis and various other inflammatory conditions.

Sirtuinmodulator 8 is a modulator of silent information regulator proteins (sirtuins) that activates their activity. It significantly reduces the expression of monocyte chemoattractant protein-1 (MCP-1) while enhancing the expression of fibroblast growth factor 21 (FGF21). Sirtuinmodulator 8 regulates the expression of genes related to inflammation and metabolism, showing potential for research into metabolic diseases [such as diabetes and obesity] and inflammatory diseases.

HSP90α-IN-1 is an HSP90α inhibitor (IC50= 111 nM) that demonstrates anti-aging activity across various cellular senescence models. Belonging to the xanthine family, HSP90α-IN-1 is involved in research focused on combating age-related inflammation, senescence, and diseases (including cancer), and it may contribute to extending healthy lifespan.

c-Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. It suppresses inflammation in J774A.1, RAW264.7, MPMs cells, and lung tissue by blocking LPS-induced NF-κB pathway activation. Additionally, c-Kit-IN-9 demonstrates effective anti-inflammatory activity in mouse models of acute lung injury and sepsis. It is useful for research on acute lung injury and related inflammatory diseases.

BCX-3607 is an orally active tissue factor/factor VIIa (TF-FVIIa) inhibitor with an IC50 of 4 nM. By inhibiting the TF-FVIIa complex, it effectively blocks the extrinsic coagulation pathway and significantly prolongs prothrombin time (PT). BCX-3607 exhibits higher selectivity for TF-FVIIa over other serine proteases like thrombin and FXa. It reduces thrombus weight and inflammation, offering dual anti-thrombotic and anti-inflammatory effects. BCX-3607 is applicable in research on thrombosis-related diseases.

FABP4-IN-3 (Compound C3) is a highly selective inhibitor of FABP4, with an inhibition constant (Ki) of 25 ± 3 nM for FABP4 and a Ki of 15.03 μM for FABP3, showcasing a selectivity factor of 601 times over FABP3. It also demonstrates metabolic stability and potent anti-inflammatory activity in cells, making it a promising candidate for research in metabolic disorders, cardiac dysfunction, and inflammation-related diseases.