1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats[1].
1,1-Dimethylurea-d6 is the deuterium labeled 1,1-Dimethylurea[1].
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately[1].
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration[1].
N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM[1].
PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC50 of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression[1].
Sultopride-d5 (LIN-1418-d5) is the deuterium labeled Sultopride. Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor[1][2].
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].
MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively[1].
Eckol is a potent hMAO-A (Mixed) and hMAO-B (non-competitive) inhibitor with IC50s of 7.20 and 83.44 μM, respectively. Eckol shows stimulatory effects in maize and can be used as a plant biostimulant. Eckol also shows antiallergic and antiviral effects[1][2][3][4].
Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest[1].
Calicheamicin is a cytotoxic agent that causes double-strand DNA breaks.
3-Methoxyflavone is a flavonoid compound isolated from Artemisia incanescens with antiviral activity[1][2].
16:0-18:0-16:0 TG-d5 is deuterium labeled 16:0-18:0-16:0 TG.
Methyl N-(1,1-dioxidotetrahydro-3-thienyl)glycinate hydrochloride is a Glycine (HY-Y0966) derivative[1].
1-Bromoundecane-d3 is the deuterium labeled 1-Bromoundecane[1].
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential[1].
Clodronic acid is an orally active bisphosphonate, which is used for researching osteoporosis and diseases associated with excessive bone resorption. Clodronic acid inhibits bone resorption through induction of osteoclast apoptosis. Clodronic acid is effective in the maintenance or improvement of bone mineral density[1].
(2R,3S,5R)-2-(hydroxymethyl)-5-(6-methyl-9H-purin-9-yl)tetrahydrofuran-3-ol (9-(2-Deoxy-beta-D-ribofuranosyl)-6-methylpurine) is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
(R)-(-)-1,2-Propanediol is a (R)-enantiomer of 1,2-Propanediol that produced from glucose in Escherichia coli expressing NADH-linked glycerol dehydrogenase genes[1].
BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1)[1].
Xanthone is isolated from Mangosteen and is known to control cell division and growth, apoptosis, inflammation, and metastasis in different stages of carcinogenesis. Xanthone has anti-oxidant, anti-tumor, anti-allergic, anti-inflammatory, anti-bacterial, anti-fungal, and anti-viral activities[1].
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
FEN1-IN-3 (Compound 4) is a human flap endonuclease-1 (hFEN1) inhibitor. FEN1-IN-3 stabilizes hFEN1 with an EC50 of 6.8 μM[1].
2-((tert-Butoxycarbonyl)amino)-3-(4-chlorophenyl)propanoic acid is a phenylalanine derivative[1].
Mca-Pro-Leu is a tripeptide[1].
Defensin NP-3A (NP-3A; Corticostatin 1) is a human granulocyte peptide, with anti-ACTH activity. Defensins are antimicrobial peptides with and cytotoxic activity[1][2].
5-FAM-LL-37 is afluorescent labeled LL-37, human (HY-P1222).