Colitis

10-Gingerol (Standard) is the analytical standard of 10-Gingerol (HY-N0448). This product is intended for research and analytical applications. 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC₅₀ value of 10.47 μM against DPPH radical, an IC₅₀ value of 1.68 μM against superoxide radical and an IC₅₀ value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC₅₀ of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis.

EP4 receptor agonist-4 is an orally active, selective EP4 receptor agonist, with a binding IC₅₀ of 18 nM against human receptors, and agonistic EC₅₀ values of 2.1 nM and 0.11 μM against human and murine receptors, respectively. EP4 receptor agonist-4 inhibits hERG channel activity with an IC₅₀ of 10.2 μM. It can be used in the research of inflammatory bowel disease (colitis).

Ambrosin is an orally active NF-κβ and BACE1 inhibitor. Ambrosin reduces pro-inflammatory and nitrosative mediators, increases PPARγ levels, inhibits apoptosis (Apoptosis), enhances autophagy (Autophagy), and ameliorates oxidative stress. Ambrosin reduces Amyloid plaque deposition. Ambrosin improves lipopolysaccharide-induced memory impairment and colonic histopathological changes. Ambrosin can be used in research related to Alzheimer's disease and colitis.

MAPK-IN-8 is an orally active MAPK inhibitor. MAPK-IN-8 can restore the balance of gut microbiota, inhibit M1 macrophage polarization and suppress MAPK mediated inflammation. MAPK-IN-8 can be used in ulcerative colitis research.

NF-κB/STAT3/iNOS-IN-1 is a NF-κB/STAT3/iNOS inhibitor. NF-κB/STAT3/iNOS-IN-1 reduces the expression of inflammatory mediators TNF-α, IL-1β, IL-6, IL-8 and COX-2. NF-κB/STAT3/iNOS-IN-1 upregulates the expression of epithelial barrier-related proteins E-cadherin, Occludin and Zonula occludens-1. NF-κB/STAT3/iNOS-IN-1 alleviates disease severity and histopathological damage in mouse colitis models. NF-κB/STAT3/iNOS-IN-1 can be used for the research of inflammatory bowel disease (colitis).

Natural indigo extract is an extract of Polygonum tinctorium that can be used in research on colitis.

(±)-10-Gingerol is the racemic form of 10-Gingerol (HY-N0448). 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC₅₀ value of 10.47 μM against DPPH radical, an IC₅₀ value of 1.68 μM against superoxide radical and an IC₅₀ value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC₅₀ of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol can be used in research on various common cancers such as ovarian cancer and colon cancer, as well as colitis and neurodegenerative diseases.

DOPE GMP is DOPE (HY-112005) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DOPE (Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine) is an orally active inhibitor of ferroptosis with anti-inflammatory and intestinal barrier maintenance activities. DOPE regulates the expression of ACSL4, SLC7A11 and GPX4 to restore the redox system balance, thereby reducing the levels of lipid peroxides, iron ions and intestinal inflammatory factors (IL-1β and IL-6). DOPE promotes the migration and proliferation of intestinal epithelial cells and increases the level of tight junction proteins; it also destabilizes endosomal membranes, mediates the conjugation of RVG peptides with mesenchymal stem cell-derived exosomes to enhance brain targeting. DOPE can be applied to research related to neonatal necrotizing enterocolitis and Alzheimer's disease.

5-Norbornene-2-methylamine-C10-NH2 is a Keap1-targeting hydrophobic tag (HyT)-linker conjugates, containing a HyT (HY-W022007) and a linker (HY-W014831). 5-Norbornene-2-methylamine-C10-NH2 can be used for synthesis of NBE5 (HY-181907).

NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).

S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC₅₀ values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease.

24-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum.

HDAC6-IN-71 (Compound 24) is a HDAC6 inhibitor with IC₅₀ values for HDAC6 and HDAC1 of 13.68 and 443.12 nM respectively. HDAC6-IN-71 effectively inhibits the production of NO by mouse macrophages, with its IC₅₀ being 2.31 μM. HDAC6-IN-71 inhibits the HDAC6-NF-κB signaling pathway, reduces the levels of phosphorylated IκB-α and IKK-α/β, and suppresses the expression of downstream inflammatory proteins COX-2 and iNOS. HDAC6-IN-71 significantly alleviates ulcerative colitis in mice.

HDAC3 degrader-1 (Compound Z8) is a selective HDAC3 degrader with a DC₅₀ of 2.42 μM. HDAC3 degrader-1 has almost no effect on HDAC1, HDAC2, and HDAC6. HDAC3 degrader-1 inhibits the activation of the NLRP3 inflammasome and reduces the secretion of IL-1β and caspase-1. HDAC3 degrader-1 shows significant efficacy in septic shock and colitis models. HDAC3 degrader-1 can be used in anti-inflammatory research.

NIK-IN-3 is a potent and orally active NF-κB-inducing kinase (NIK) inhibitor with an IC₅₀ of 5.2 nM. NIK-IN-3 suppresses non-canonical NF-κB pathway activation and inhibits the secretion of pro-inflammatory cytokines, such as TNF-α, IL-6, IL-1β and chemokine CXCL12. NIK-IN-3 shows significant anti-inflammatory effects in LPS (HY-D1056)-induced sepsis mice model and DSS (HY-116282)-induced colitis model. NIK-IN-3 can be used for the research of inflammation, such as colitis.

Dihydrocoptisine is a benzylisoquinoline alkaloid that can be isolated from the methanolic extract of the whole plant of Argemone mexicana L. Dihydrocoptisine can activate XBP1 transcription activity. Dihydrocoptisine can be studied in research on anti-ulcertative colitis.

N-Cholyl-L-aspartic acid (AspCA) is a N-cholyl Amino Acid (HY-168761) derivative. N-Cholyl-L-aspartic acid can be used for the study of inflammatory bowel disease (IBD).

EP4 receptor agonist 3 prodrug (Compound 9) is a prodrug of EP4 receptor agonist (Compound 1a). EP4 receptor agonist 3 prodrug itself has no agonistic activity on the EP4 receptor and needs to be specifically hydrolyzed by intestinal alkaline phosphatase (IAP) in the intestine to release the active molecule, which then exerts the EP4 receptor agonistic effect locally in the intestine. EP4 receptor agonist 3 prodrug has colonic targeting properties and significantly alleviates colitis in mice.

Orazipone (OR 1384) is a small molecule immunomodulator with strong anti-inflammatory properties. Orazipone exerts its immunomodulatory effect by forming reversible thiol complexes, which bind to intracellular signaling proteins and the thiol groups of glutathione. Orazipone exhibits potent anti-eosinophilic activity by inducing apoptosis. Orazipone inhibits activation of inflammatory transcription factors NF-kB and STAT 1 and decreases inducible iNOS expression and NO production in response to inflammatory stimuli. Orazipone reduces NADPH oxidase activity and thereby decreases ROS production. Orazipone has a protective effect in intestinal radiation injury.

15-PGDH-IN-4 (Compound 40) is a 15-PGDH inhibitor with an IC₅₀ of 1.2 nM against h15-PGDH. 15-PGDH-IN-4 functionally inhibits the activity of 15-PGDH. 15-PGDH-IN-4 can be used in the research of colitis.