inflammatory bowel disease

Declopramide (OXI-104) is a novel chemosensitizer with antitumor activity that induces apoptosis and can be used to study colorectal cancer and inflammatory bowel disease.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

Oxazolone has been used as a haptenizing agent, which can induce an inflammatory reaction in adult zebrafish intestinal tissues and this can be used as a model for gene expression studies of the two forms of inflammatory bowel disease like Crohn's disease

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.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Dextran sulfate sodium salt (MW 4500-5500) is an anhydrous glucose polymer with a molecular weight range of 4500-5500. It inhibits human immunodeficiency virus replication by preventing viral adsorption to host cells and is commonly used to model inflammatory bowel disease. The high negative charge from its sulfate groups damages the intestinal mucosal barrier, leading to intestinal barrier dysfunction, macrophage impairment, and bacterial flora disorder.

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.

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

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

SC-22716 is an orally active leukotriene A4 (LTA4) hydrolase inhibitor.SC-22716 has potential anti-inflammatory activity and may be used in the study of inflammatory bowel disease and psoriasis.

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

GPR183 (3-(3,4-difluorophenyl)-N-[3-fluoro-5-(morpholin-4-yl)phenyl]propanamide) is a chemotactic receptor known for its role in the maturation of B cells, and the endogenous ligand is the oxysterol 7α,25-dihydroxycholesterol (7α,25-OHC). GPR183 can be used in research on inflammatory bowel disease (IBD).

PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM [1].

Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

Sibofimloc (Antibiotic-202), an antibiotic compound, is used in treating bacterial infections.

Tazofelone (LY-213829) is a NSAID used for the treatment of inflammatory bowel disease.

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

Dalazatide (ShK-186) is a specific inhibitor of the Kv1.3 potassium channel, used in research on autoimmune conditions such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease [1] [2] [3].

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

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, exhibiting a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].

Elubrixin tosylate (SB-656933 tosylate) is a high-potency, selective, competitive, and reversible CXCR2 and IL-8 receptor antagonist. It effectively inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). This compound holds promise for studying inflammatory diseases, including inflammatory bowel disease and airway inflammation.

ABT-510 acetate is an endogenous anti-angiogenic TSP peptide inhibitor, a thrombospondin analog, with anti-inflammatory, anti-cancer and anti-angiogenic activity that induces apoptosis and inhibits ovarian tumor growth in an orthotopic, syngeneic model of epithelial ovarian cancer.ABT-510 acetate reduces angiogenesis and inflammatory responses in a mouse model of inflammatory bowel disease. ABT-510 acetate reduces angiogenesis and inflammation in mouse models of inflammatory bowel disease (IBD) and can be used in cancer research, particularly in epithelial ovarian cancer, as well as in inflammatory bowel disease (IBD).

Hispidol ((Z)-Hispidol) ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 μM.

Prednisolone sodium metazoate is used in the treatment of Inflammatory Bowel Disease, Ulcerative Colitis, and GI Disorders.

Etrolizumab (rhuMAb Beta7), a gut-selective anti-β7 integrin monoclonal antibody, targets the β7 subunit of α4β7 and αEβ7 integrins specifically, demonstrating affinity with K i values of 18 nM for Human α4β7 and 1800 pM for Human αEβ7-293. It is utilized in the research of inflammatory bowel disease (IBD) [1] [2].

PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist, with K i values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. For rat and human A1 receptors, it has significantly lower affinity, with K i values of ≥10000 nM and 541 nM, respectively. The compound exhibits poor brain penetration and is not orally absorbable. It is of interest in research related to inflammatory bowel disease (IBD) [1] [2] [3].

NLRP3-IN-37 (Compound 23), an NLRP3 inhibitor (EC50: 5 nM), can be used for research on NLRP3-related conditions, including gout, pseudogout, CAPS, NASH fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease, and traumatic brain injury [1].

Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

Dolcanatide, an orally active guanylate cyclase-C (GC-C) agonist, exhibits laxative, anti-nociceptive, and anti-inflammatory properties. It is utilized in research concerning inflammatory bowel disease [1] [2].

PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor with an IC50 of 15 nM, exhibiting anti-inflammatory properties through the inhibition of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 expression induced by LPS. It has demonstrated efficacy in mitigating inflammatory bowel disease (IBD) symptoms in a dextran sodium sulfate (DSS)-induced colitis mouse model, suggesting its potential utility for IBD research [1].

hDHODH-IN-13 (compound w2), an inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibits an IC50 of 173.4 nM and has potential research applications in studying inflammatory bowel disease (IBD) [1].

E6130 may be effective in the treatment of inflammatory bowel disease and is a highly selective CX3CR1 regulator for oral administration.

Recflavone( DA-6034) is a synthetic derivative of eupatilin and flavonoids that have anti-inflammatory effects against inflammatory bowel disease.

Tetomilast (OPC-6535) is a phosphodiesterase-4 (PDE4) inhibitor, potentially effective for treating inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).

ALB-127158(a) is a potent and selective melanin-concentrating hormone 1 (MCH 1) receptor antagonist that may potentially treat inflammatory bowel disease (IBD).

NLRP3-IN-12 is a specific inhibitor of the NLRP3 inflammasome that targets the NLRP3 protein to effectively reduce IL-1β release, with an IC50 of 0.45 μM. This compound is utilized in the research of inflammatory bowel disease (IBD).

RR-RJW100, an enantiomer of RJW100, functions as an agonist for both nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). Among its two synthesized enantiomers, RR-RJW100 and SS-RJW100, the former exhibits greater potency as an LRH-1 agonist. This compound plays a crucial role in regulating metabolic homeostasis and is utilized in researching diabetes, liver disease, and inflammatory bowel disease.

CRA-2059 is a highly specific and selective tryptase inhibitor with a Ki of 620 pM for recombinant human tryptase-β (rHTβ) [1][2].

CU06-1004 (Sac-1004) is an orally active compound that mitigates endothelial dysfunction by inhibiting hyperpermeability and inflammation. It reduces vascular leakage and inflammation in multiple animal models, including diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. CU06-1004 also improves conditions in a CDAA-induced mouse model of NASH and enhances cardiac function [1] [2] [3].

DC-SX029 is a potent inhibitor of SNX10 protein-protein interaction (PPI) with an estimated K D constant of approximately 0.935 μM as measured by surface plasmon resonance (SPR). It blocks the SNX10-PIKfyve interaction, leading to decreased TBK1 c-Rel signaling activation, without affecting SNX10 protein levels. DC-SX029 shows potential for inflammatory bowel disease (IBD) research [1].

Briakinumab (ABT-874), a fully human anti-IL-12/23p40 monoclonal antibody, selectively targets and neutralizes IL-12 and IL-23. This compound is utilized in the research of various autoimmune disorders, including rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis [1].

Abrilumab, a fully human monoclonal antibody, targets the α4β7 integrin heterodimer, selectively binding to it. This specificity makes it a potential research tool for investigating inflammatory bowel disease (IBD) [1].

Zharp2-1, a RIPK2 inhibitor, inhibits the transcription of inflammatory cytokines induced by MDP-induced or Listeria monocytogenes infection and alleviates MDP-induced peritonitis symptoms in mice, which can be used for the study of inflammatory bowel disease (IBD).

A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma

Vidofludimus hemicalcium (4sc-101; SC12267) is an orally active compound that acts as a dihydroorotate dehydrogenase (DHODH) inhibitor and serves as a novel modulator of the farnesoid X receptor (FXR). This immunomodulatory agent is utilized in the research of autoimmune disorders, including inflammatory bowel disease (IBD), and is explored for its potential in fatty liver disease research through FXR targeting.

RORγt DHODH-IN-2 (compound 1) is a potent dual inhibitor of RORγt and DHODH, useful for studying inflammatory bowel disease (IBD).