13-cis Acitretin D3 （Isoacitretin D3） is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis[1][2].
Allosecurinine (Phyllochrysine) is a Securinega alkaloid isolated from M.indica and M.discoidea[1].
Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities[1].
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects[1][2].
Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities[1].
Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
Mofebutazone, a monophenyl analogue of Phenylbutazone (DPB), is an anti-inflammatory compound. Mofebutazone can be used for research of asthma[1][2].
Tr-PEG4-OH is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
AMG 487 is an antagonist of chemokine receptor 3 CXCR3 which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
RDR 03785 is a covalent MIF inhibitor with an IC50 of 0.36 μM[1].
Antituberculosis agent-7, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis with a MIC of 31.25 μM. Antituberculosis agent-7 shows good antifungal activity against A. niger with a MIC of 62.5 μM. Antituberculosis agent-7 shows excellent antimycobacterial activity with MIC 3.41 μM for M. tuberculosis H37Rv[1].
Streptazolin is an antibiotic. Streptazolin increases bacterial killing and elaboration of immunostimulatory cytokines by macrophages in vitro. Streptazolin stimulates the macrophage NF-κB pathway via PI3K signaling[1][2].
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity[1].
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively[1][2].
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM[1].
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1].
Adalimumab (anti-TNF-α) is a human monoclonal IgG1 antibody targeting tumour necrosis factor α (TNF-α).
Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
α-Glucosidase-IN-3 is an oleanolic acid (OA) oxime ester derivative against α-glucosidase (IC50=1.28 µM) and α-amylase (IC50=3.8 µM) .
Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases.
Ganoderic acid J is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid J possesses anti-inflammatory anti-inflammatory activity[1][2].
Imiloxan is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan has the potential for acute kidney injury research[1][2].
PLP (139-151) is amino acid residue 139 to 151 of myelin proteolipid protein (PLP) used to induce experimental autoimmune encephalomyelitis (EAE).
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities[1][2].
C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
Atrazine-3-mercaptopropanoic acid is a hapten. The IC50 value of polyclonal antibody (PcAb) 1 with coating Atrazine-3-mercaptopropanoic acid is 7.5 ng/mL[1].
Rabeprazole is an antiulcer drug in the class of proton pump inhibitors.Target: Proton PumpRabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds.