Heteropeucenin 7-methyl ether is a chromone that can be found in Harrisonia perforata[1].
BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.
E3 ligase Ligand-Linker Conjugates 5 Free Base is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
Utreglutide is a potent glucagon-like peptide 1 (GLP-1) receptor agonit[1].
Xanthine oxidase-IN-9 (Icarisids E) (Compound 2) is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 31.81 μM[1].
Mogroside III-A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed.Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly.
(E)-Benzyl ferulate is a phenolic ester that can be isolated from Thai propolis[1].
Succinic anhydride-13C2 is the 13C labeled Succinic anhydride[1]. Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide[2].
(S)-Alprenolol is a potent and nonselective β-adrenoceptor antagonist[1].
5-Sulfosalicylic acid is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid is effective against the breast cancer cell line, MCF-7, with less toxicity[1]. 5-Sulfosalicylic acid has antioxidant activities[2].
Biotin-hexanamide-(L-Thyroxine) is biotinylated L-Thyroxine (HY-18341). L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism[1].
Propargyl-PEG1-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1,3-Dibromo-5,5-dimethylhydantoin is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase ((DYRK)) inhibitor with anticancer and anti-inflammatory activities.
S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation[1][2][3].
(Rac)-RK-682, a racemate of RK-682, is a protein tyrosine phosphatases (PTPases) inhibitor. (Rac)-RK-682 inhibits protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B) with IC50s of 8.6 μM, 12.4 μM, and 0.7 μM, respectively[1].
GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM.
Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.Target: AChEDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration [2]. A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases [3].
Fmoc-Methylalanine-d3 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Xanthopurpurin, an anthraquinone glycoside, isolated from the roots of Rubia akane, shows mainly strong inhibition of collagen-induced platelet aggregation[1].
Ald-CH2-PEG3-azide is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer[1].
E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
N-(Amino-PEG3)-N-bis(PEG4-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Laurolitsine ((+)-Norboldine) is an alkaloid isolated from the leaves of Peumus boldus Molina[1].
Vertilmicin Sulfate, an aminoglycoside antibiotic, is used potentially for the treatment of bacterial infections.
Mouse TREM-1 SCHOOL peptide (Mouse TREM-1(213-221), GF9) targets interactions between TREM-1 and its signaling partner DAP-12, and inhibits TREM-1 signaling. Mouse TREM-1 SCHOOL peptide has antitumor effect[1].
SOS1/KRAS-IN-1(Compound 2) is a SOS1/KRAS inhibitor, which can be used in the research of SOS1/KRAS-mediated diseases[1].
Asiaticoside B is a triterpene glycoside isolated from Actaea asiatica, with anti-cancer activity[1].