Benzydamine N-Oxide is a metabolite of Benzydamine. Benzydamine N-Oxide can be used to measure flavin-containing monooxygenase activity[1][2].
WRW4-OH is a biological active peptide. (This peptide inhibits binding of one of formyl peptide receptor-like 1 (FPRL1) agonists WKYMVm to its specific receptor. FPRL1 is an important classical chemoattractant receptor that is expressed in phagocytic cells in the peripheral blood and brain. Activation of FPRL1 is closely related to inflammatory responses in the host defense mechanism and neurodegenerative disorders.)
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.
(25R)-Officinalisnin-II (compound 5) is a furostanol glycoside found in the fruits of Asparagus curillus[1].
CID755673 is a potent and selective PKD1 inhibitor with an IC50 of 182 nM.
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker[1][2]. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia[3].
R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).
Cleomiscosin C (Aquillochin) can be isolated from Aquilaria agallocha. Cleomiscosin C has antioxidant activity. Cleomiscosin C inhibits LDL oxidation and free radicals generation[1].
Ingenol-3-palmitate, an ingenane diterpenoid, is a nature product that could be isolated from the roots of Euphorbia ebracteolata. Ingenol-3-palmitate is a potent HIV-1 (HIV) inhibitor with an IC50 value of 4.1 nM[1].
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways[1]. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons[2].
Nodosin is a diterpenoid isolated from Isodon trichocarpus Kudo and I. Japonicus HARA[1].
BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation[1].
Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM.Target: Adenosine diphosphate (ADP)Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family. Ticlopidine hydrochloride inhibits platelet aggregation with IC50 of ~2 μM in men. Like clopidogrel, it is an adenosine diphosphate (ADP) receptor inhibitor. It is used in patients in whom aspirin is not tolerated, or in whom dual antiplatelet therapy is desirable. Because it has been reported to increase the risk of thrombotic thrombocytopenic purpura (TTP) and neutropenia, its use has largely been supplanted by the newer drug, clopidogrel, which is felt to have a much lower hematologic risk. Its niche role as an alternative in those patients who do not tolerate Clopidogrel has now been superdeded by Ticagrelor and Prasugrel. The usual dose is 250 mg twice daily by the oral route.Ticlopidine hydrochloride, when orally administered to rats, results in activation of basal and prostaglandin E1 (PGE1)-stimulated adenylate cylase activity through increase in affinity of the cyclase in platelet membrane to PGE1, although it failed to affect adenosine- or sodium fluoride-stimulated activity of the enzyme.
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as green onion (Allium cepa) or noni (Morinda citrifolia L.) leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins[1].
Depressine is a natural product found in Gentiana depressa[1].
Fmoc-D-Phe(2-F)-OH is a phenylalanine derivative[1].
Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure[1].
Angeloylgomisin O, a lignin extract of Schisandra rubriflora. Anti-inflammatory properties[1].
BiP substrate is a peptide substrate of BiP that can be used to measure the BiP ATPase activity[1].
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Polyinosinic-polycytidylic acid presents in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA.
Amino-PEG9-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(S)-MCPG is the active isomer of (RS)-MCPG (Cat. No. HY-100371), non-selective group I/group II metabotropic glutamate receptor antagonist. In vivo: (S)-MCPG (20.8 μg) injected intraventricularly (i.c.v.) before testing impaired the performance of rats in the spatial version of the Morris water maze, but 1/10 of this dose did not. Memory retention, evaluated 24 hr post-training, is also affected by the high dose of MCPG.
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2].
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice[1].
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1].
Kinetin (N6-furfuryladenine) belongs to a group of plant growth hormones involved in cell division, differentiation and other physiological processes.IC50 Value: Target:Kinetin is one of the widely used components in numerous skin care cosmetics and cosmeceuticals, such as Valeant products kinerase. Recently, kinetin has the potential to be a treatment for the human splicing disease familial dysautonomia.in vitro: Kinetin-induced cell death reflected by the morphological changes of nuclei including their invagination, volume increase, chromatin condensation and degradation as well as formation of micronuclei showed by AO/EB and 4,6-diamidino-2-phenylindol staining was accompanied by changes including increase in conductivity of cell electrolytes secreted to culture media, decrease in the number of the G1- and G2-phase cells and appearance of fraction of hypoploid cells as the effect of DNA degradation without ladder formation [1]. The plant cytokinin kinetin dramatically increases exon 20 inclusion in RNA isolated from cultured FD cells [3].in vivo: Subjects received 23.5 mg/Kg/d for 28 d. An increase in WT IKBKAP mRNA expression in leukocytes was noted after 8 d in six of eight individuals; after 28 d, the mean increase compared with baseline was significant (p = 0.002) [2].Toxicity: On mice with leukaemia P388, kinetin has no effect on the tumour growth, and it appears to be toxic at the dose of 25 mg/kg [4].
Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
Carabersat is a potent anticonvulsant agent.