inflammatory bowel disease (ibd)

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Dextran sulfate sodium salt (MW 36,000–50,000) is a medium molecular weight polyanionic dextran derivative with strong intestinal epithelial permeability. It is the most commonly used agent for inducing inflammatory bowel disease (IBD) models, effectively inducing both acute and chronic colitis. Its mechanism may involve macrophage dysfunction and gut microbiota dysbiosis. Due to its colonic epithelial toxicity, long-term use can also induce colorectal cancer models.

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.

ZK 216348 is a non-steroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to progesterone receptors and mineralocorticoid receptors with IC₅₀ values of 20.4 nM and 79.9 nM, respectively, and may be useful for studying inflammatory bowel disease (IBD).

NS6180 is a potent and selective KCa3.1 channel inhibitor(IC50= 9 nM). It prevents T-cell activation and inflammation.

L-Homocysteine is a biological thiol involved in various diseases and pathological conditions. It is a marker for atherosclerosis and can exacerbate intestinal inflammation in inflammatory bowel disease (IBD) by promoting the expression of 5-LOX and COX-2, making it suitable for inducing vascular endothelial inflammation models.

D228, a natural product from Chimonanthus salicifolius, is an orally available anti-inflammatory agent with favorable inhibitory activity on B and T lymphocytes, down-regulation of MyD88/TRAF6/p38 and up-regulation of IL-10 to reduce inflammation, and can be used for the treatment of inflammatory bowel disease (IBD).

CDK8/19-IN-3 (compound 3-7) is a potent and selective inhibitor of CDK8 and CDK19. It can increase IL-10 levels and has potential for research in inflammatory bowel disease (IBD).

5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory properties. It suppresses IL-6, IL-1β, TNF-α, and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. Additionally, 5-LOX-IN-8 decreases the disease activity index in DSS colitis models. This compound is applicable for research in inflammatory bowel disease (IBD).

Quin-C7 is an orally active FPR2/ALX antagonist with anti-inflammatory properties. It demonstrates efficacy in ameliorating DSS-induced colitis in mice and is suitable for research in inflammatory bowel disease [IBD].

NLRP3-IN-76 is an orally active NLRP3 inhibitor that suppresses the production of NO and reduces the mRNA levels of pro-inflammatory cytokines (iNOS, IL-6, IL-1β, and TNFα). It exerts anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome and the NF-κB signaling pathway. Furthermore, NLRP3-IN-76 can ameliorate DSS-induced colitis and is applicable for studying inflammatory bowel disease (IBD).

NLRP3-IN-75 is an orally effective inhibitor of NLRP3, capable of suppressing IL-1β secretion with an IC50 of 23 nM. It selectively inhibits NLRP3 activation by disrupting inflammasome assembly without affecting the assembly of NLRC4 or AIM2 inflammasomes. NLRP3-IN-75 demonstrates excellent anti-inflammatory effects in models of acute peritonitis, diabetic nephropathy, and inflammatory bowel disease (IBD).

METTL3-IN-7 (F039-0002) is a potent inhibitor of METTL3. It significantly ameliorates colitis induced by dextran sulfate sodium (DSS) and is applicable for research in inflammatory bowel disease (IBD).

CXCR4-IN-3 (compound XVI) is an orally active inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. It exhibits potent anti-chemotactic effects, with an inhibition rate of 79.19±2.33%. Additionally, CXCR4-IN-3 possesses anti-inflammatory properties and can be utilized in research on IBD (inflammatory bowel disease).

Anti-inflammatory agent 86 is a derivative of Chrysin with anti-inflammatory properties. It inhibits TNF-α-induced monocyte adhesion to colon epithelium, with an IC50 of 4.71 μM. Anti-inflammatory agent 86 shows potential for use in inflammatory bowel disease (IBD) research.

GS-1427 (Emvistegrast) is a quinolone derivative and integrin α4β7 antagonist for studying α4β7 integrin-mediated diseases such as inflammatory bowel disease (IBD).

Spns2-IN-3 (compound 510) is an SPNS2 inhibitor with an IC50 value of 1.2 μM for hSPNS2. It is applicable in research on autoimmune diseases such as multiple sclerosis (MS) and inflammatory bowel disease (IBD), as well as fibrosis, muscle atrophy, metastasis, acute lung injury, rheumatoid arthritis, colitis, Alzheimer's disease, and other conditions linked to SPNS2 activity.

RORγt inverse agonist 35 (Compound 22) is an RORγt inverse agonist with an IC50 of 1.51 μM. It significantly inhibits Th17 differentiation and pro-inflammatory characteristics in human CD4+ T cells. This compound can be utilized for research on Th17-driven autoimmune diseases, such as psoriasis, multiple sclerosis, and inflammatory bowel disease (IBD).

KB-0118 (BBC0115) is an inhibitor targeting the BET bromodomain. It selectively binds to BRD2 and BRD4, with dissociation constants (Kd) of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1, while not binding to BRD3. KB-0118 suppresses the secretion of pro-inflammatory cytokines such as TNF, IL-1β, and IL-23a, and selectively inhibits Th17 cell differentiation. The compound regulates Th17-driven inflammation through the epigenetic suppression of BRD4, as evidenced by the downregulation of STAT3 and BRD4 target genes. Additionally, KB-0118 exhibits immunomodulatory effects in inflammatory bowel disease (IBD) models.

Indolimine-214 is a metabolite of M. morganii. It elevates γH2AX levels in HeLa cells and is applicable in research on inflammatory bowel disease (IBD) and colorectal cancer (CRC).

sEH-IN-21 is an orally active inhibitor of sEH, exhibiting IC50 values of 0.1 nM for both hsEH and msEH. It significantly suppresses the NF-κB signaling pathway. sEH-IN-21 demonstrates potent anti-inflammatory activity by reducing IL-6 and TNF-α release and maintaining intestinal barrier integrity. It is applicable in research on inflammatory bowel disease (IBD).

HW201877 is a potent, orally active inhibitor of 15-prostaglandin dehydrogenase (15-PGDH), with an IC50 value of 3.6 nM. It significantly increases PEG2 levels in A549 cells and demonstrates notable efficacy in animal models of tissue injury and fibrosis. HW201877 is utilized in research for inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF), and Crohn's disease (CD).

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor with an IC50 of less than 10 nM and demonstrates high selectivity over MMP-1, -2, -3, -7, -9, -10, and -14. It significantly reduces lung fibrosis in a mouse model of bleomycin-induced unilateral pulmonary fibrosis and effectively alleviates kidney damage, interstitial inflammation, or fibrosis in a unilateral ureteral obstruction renal fibrosis model. Linvemastat is suitable for research into inflammatory diseases such as idiopathic pulmonary fibrosis (IPF), inflammatory bowel disease (IBD), and asthma.

PHD2-IN-6 (Example 89) is an inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 31.6 nM. This compound can stimulate the production of the gene encoding erythropoietin (EPO). PHD2-IN-6 is applicable in research on inflammatory diseases such as inflammatory bowel disease (IBD) and rheumatoid arthritis.