Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.

Allura Red AC (CI 16035) is a very important food azo dye used in the food, pharmaceutical, paper, cosmetic and textile industries.Allura Red AC promotes susceptibility to experimental colitis via mouse intestinal serotonin.

DL-Methionine Methylsulfonium Chloride is a natural product, used in the treatment of peptic ulcers, colitis, and gastritis.

5-Acetylsalicylic acid (5-acetyl-2-hydroxybenzoic acid) has anti-inflammatory effects and can be used to treat inflammatory bowel disease, including ulcerative colitis, inflamed anus or rectum, and to maintain remission in Crohn's disease.

Ozanimod hydrochloride (RPC-1063 hydrochloride) is an orally available, selective and potent sphingosine 1-phosphate (S1P) receptor modulator that shows high affinity for S1P1 and S1P5.Ozanimod has potential anticancer activity and can be used in the study of multiple sclerosis (MS), ulcerative multiple sclerosis (UMS), and other diseases. (MS), ulcerative colitis, coronavirus infections and myelodysplasia.

4-methoxylonchocarpin was isolated from the roots of Abrus precatorius as a potent anti-inflammatory compound. 4-methoxylonchocarpin inhibited NF-κB-activated TNF expression by inhibiting the binding of LPS to TLR4 in macrophages and suppressed TNBS-induced colitis in mice.

MoTPS1-IN-1 is a potent MoTPS1 inhibitor with antifungal and potentially anti-inflammatory activity that acts through interaction with Glu396 and can be used to study ulcerative colitis.

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

Cilansetron is an effective and selective 5-HT3 receptor antagonist that can be used for related diseases caused by colitis.

Dersalazine (Dersalazine Free Base), an inhibitor of platelet-activating factor, exerts intestinal anti-inflammatory activity in different rodent types of colitis by down-regulating IL-17 expression, with potential efficacy in patients with ulcerative colitis.

P-2281 is an mTOR inhibitor with anticancer and anti-inflammatory properties.P-2281 inhibits dextran sulfate sodium (DSS)-induced colitis by suppressing T-cell function and is effective in a mouse model of human colitis.

P32/98 hemifumarate is a dipeptidyl peptidase IV (DPP4) inhibitor with hypoglycemic properties that improves insulin sensitivity and β-cell responsiveness in the Zucker diabetic rat model, and may be useful in studies of type 2 diabetes and colitis.

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

Pyrrolidinedithiocarbamate ammonium (1-Pyrrolidinedithiocarboxylic acid ammonium salt), a selective NF-κB inhibitor, inhibits translation of nitric oxide synthase mRNA to prevent induction.

CTP-NBD is a cell-permeable, specific inhibitor of the NFκB peptide, which has been utilized in studies of colitis [1] [2].

hCES2-IN-1 (Compound 24) is a reversible, selective inhibitor of the human carboxylesterase 2 (hCES2) enzyme, exhibiting an IC50 of 6.72 μM. This compound diminishes hCES2 levels in vivo and demonstrates efficacy in alleviating irinotecan-induced delayed diarrhea and DSS-induced ulcerative colitis [1].

Teupolioside is a putatively ameliorates colitis that is isolated from Ajuga reptans.

3,4-O-Isopropylidene-shikimic acid (3,4-O-Isopropylidene shikimic acid) has significant anti-inflammatory, anti-thrombosis, antioxidant, analgesic effects, it has protective effects on experimental colitis induced by trinitrobenzenesulfonic acid in rats, probably due to antioxidant action.

1. Tussilagone inhibits dendritic cell function through the induction of heme oxygenase-1. 2. Tussilagone has anti-cancer activity, might be a potential chemotherapeutic agent for the prevention and treatment of human colon cancer. 3. Tussilagone has anti

Human β-defensin-2 (HβD-2) is a cationic skin-antimicrobial peptide (SAP) characterized by its small size and rich cysteine content. It is produced by various epithelial cells and exhibits potent antimicrobial properties against gram-negative bacteria and Candida. However, it does not effectively target gram-positive Staphylococcus aureus. Given these characteristics, Human β-defensin-2 serves as a valuable tool in colitis research.

Tesnatilimab is a potent humanized IgG4 monoclonal antibody that binds to the immune-activating receptor NKG2D. Tesnatilimab has potential immunomodulatory and anti-inflammatory activity and can be used to study active ulcerative colitis.

Antimicrobial agent-21 is a potent mitogen activated protein kinase inhibitor with antibacterial, anti-inflammatory and antitumor activity for the treatment of cataracts, ulcerative colitis, meningitis and Kawasaki's disease and Parkinson's disease.

Tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate inhibit of human recombinant EGLN-1 as substrate after 20 mins by mass spectrophotometric analysis.

1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta. 1,3,5,8-Tetrahydroxyxanthone has antispasmodic effect and anti-inflammatory activity. Dimethylbellidifolin shows mutagenicity in Salmonella typhimurium TA100, TA98, TA97, and TA2637 by the preincubation method; it also exhibits at the dose of 200 ug/disk a significant inhibition of the growth of Staphylococcus aureus.

Mongersen (GED-0301), a specific and orally active SMAD7 antisense oligonucleotide, enhances TGF-β1 activity, reducing inflammatory signals. It has been shown to alleviate experimental colitis resembling Crohn's disease in mice [1] [2].

Eldelumab (BMS-936557) is a humanized anti-IP-10 IgG type 1 monoclonal antibody with inhibitory activity against CXCL10.Eldelumab has anti-inflammatory activity and selectively binds to CXCL10 and can be used in the study of rheumatoid arthritis, ulcerative colitis, and Crohn's disease.

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy for ulcerative colitis[1].

Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of Crohn's disease and ulcerative colitis.

Anti-inflammatory agent 51 is an amide/sulfonamide derivative with anti-inflammatory and potentially anti-tumor activity and inhibition of NF-κB activation, which can be used to study acute lung injury and ulcerative colitis.

HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory properties by reducing mRNA levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and MCP-1). Additionally, it potentiates the anti-inflammatory effects of orthosteric agonists in a mouse model of colitis [1].

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)

Aprofene (Aprophen) is an antagonist of muscarinic and nicotinic acetylcholine receptors. It may be used in the therapy of peptic ulcers, endarteritis (inflammation of the inner shell of the artery), cholecystitis (inflammation of the gallbladder), and sp

Olsalazine disodium (Dipentum) is bioconverted to 5-aminosalicylic acid (5-ASA) in the colon and has anti-inflammatory activity in ulcerative colitis.

NLRP3-IN-4 is a highly efficient and orally bioavailable inhibitor of NLRP3 inflammasome, which exhibits strong anti-inflammatory properties specifically targeted towards colitis.

BTZO-15 is a novel ARE activator, ameliorating DSS- and TNBS-induced colitis in rats.

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

PAD-IN-2 is a potent inhibitor of pad4 with an IC50 value <1 μM and can be used to study autoimmune diseases and cancers such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, cystic fibrosis, ulcerative colitis, asthma, multiple sclerosis, and psoriasis.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Carotegrast methyl (AJM300), an orally-active small molecule, can antagonize the α4 integrin receptor. It is a specific and dual α4β1/α4β7 integrin antagonist.

Olsalazine (Dipentium), an anti-inflammatory drug, is used in the treatment of inflammatory bowel disease. It is also a novel DNA hypomethylating agent.

Kaurenoic acid (kaurenoate) has anti-inflammatory potential in acetic acid-induced colitis, decreases in MDA level. Kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of ATP-sensitive potassium channels. Kaurenoic acid exhibits an analgesic effect in a consistent manner and that its mechanisms involve the inhibition of cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. Kaurenoic acid derivatives have an antimicrobial activity of substituted on carbon-15 at concentrations greater than or equal to 250 μg/ml. Kaurenoic acid has inhibitory effects on the LPS-induced inflammatory response in RAW264.7 macrophages.

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.

Solcitinib (GLPG-0778) (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.

Icatibant Acetate, an antagonist of the bradykinin B2 receptor, is used in the treatment of hereditary angioedema.

1. Monotropein (Monotropeine) has antinociceptive action. 2. Monotropein has anti-apoptosis and anti-catabolic activity in chondrocytes. 3. Monotropein has anti-inflammatory action by inhibition of the expressions of inflammatory mediators via NF-κB inactivation, and support its possible therapeutic role in colitis. 4. Monotrope ininhibit the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) mRNA in LPS-induced RAW 264.7 macrophages.

SR12418 is a specific REV-ERB synthetic ligand that acts on REV-ERBα (IC50: 68 nM) and REV-ERBβ (IC50: 119 nM) and can be used to study experimental autoimmune encephalomyelitis (EAE) and colitis.

Rivanicline galactarate is a Nicotinic Receptor Agonist that may be useful in the treatment of Ulcerative Colitis.

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

LFS-829 is a a small-molecule antagonist of exportin-1. LFS-829 showed low-range nanomolar activities. Oral administration of LFS-829 can significantly reverse the pathological features of colitis model mice. LFS-829 can attenuate dual NF-κB signaling and the Nrf2 cytoprotection pathway via targeting exportin-1 in colitis mice. Moreover, LFS-829 has a very low risk of cardiotoxicity and acute toxicity. LFS-829 holds great promise for the treatment of colitis and may warrant translation for use in clinical trials.