P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease[1].
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury[1][2][3].
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc[1].
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3].
Diapocynin (Dehydrodiacetovanillone), a dimeric derivative of Apocynin, is an orally active NADPH oxidase inhibitor. Diapocynin has anti-inflammatory, neuroprotection and antioxidant activities[1].
Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
Adenylyl cyclase type 2 agonist-1 (Compound 73) is a potent agonist of adenylyl cyclase type 2 (AC2) with the EC50 of 90 nM. Adenylyl cyclase type 2 agonist-1 inhibits expression of Interleukin-6, making it a potential lead compound against respiratory diseases[1].
Oxyphenonium bromide is an antiacetylcholine compound. Oxyphenonium bromide is an antagonist of mAChR. Oxyphenonium bromide protects against the bronchial obstructive effects[1][2][3].
PIKfyve-IN-2 is a potent PIKfyve kinase inhibitor and can be used for cancers, autoimmune disorders research[1].
CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects[1].
FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorMethylprednisolone is typically used for its anti-inflammatory effects. Common uses include arthritis therapy and short-term treatment of bronchial inflammation or acute bronchitis due to various respiratory diseases. Methylprednisolone is used both in the treatment of acute periods and long-term management of autoimmune diseases, most notably systemic lupus erythematosus. It is also used for vestibular neuritis [1].After six months the patients who were treated with methylprednisolone within eight hours of their injury had significant improvement as compared with those given placebo in motor function (neurologic change scores of 16.0 and 11.2, respectively; P = 0.03) and sensation to pinprick (change scores of 11.4 and 6.6; P = 0.02) and touch (change scores, 8.9 and 4.3; P = 0.03). Benefit from methylprednisolone was seen in patients whose injuries were initially evaluated as neurologically complete, as well as in those believed to have incomplete lesions [2].
GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.
Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
Apigenin-7-diglucuronide is a flavonoid glycoside and is present in an assortment of medicinal plants with anti-inflammatory or ant-oxidant activities. Apigenin-7-diglucuronide protects retinas against bright light-induced photoreceptor degeneration through the inhibition of retinal oxidative stress and inflammation[1].
L-Lysine acetate is an essential amino acid. L-Lysine acetate can be research for vascular calcification (VC) and Acute pancreatitis[1][2].
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation[1].
(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1].
Usnoflast is a NLRP3 modulator, as well as a non-steroidal anti-inflammatory agent (NSAD)[1].
Quadrol is an immunostimulant and has been implicated as a potentially useful agent in accelerated wound healing.
4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine has the potential for the research of immune-related diseases such as cancer and autoimmune disorders[1][2].
MIF-IN-2 is a migration inhibitory factor (MIF) inhibitor extracted from patent WO2021258272A1 compound 1. MIF-IN-2 can be used for the research of immune inflammation-related diseases[1].
GB-2a is a bioflavonoids that can be isolated from Rheedia gardneriana. GB-2a has significant analgesic activity in mice with 58.9% inhibition[1].
Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals[1].
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study[1][2][3].
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS[1][2].
Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity[1].
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models[1].