Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway[1].
Pirimicarb-d6 is the deuterium labeled Diuron. Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
AA 497 is a bronchodilator[1].
Porphyra 334 is an antioxidative and anti-photoaging agent. Porphyra 334 suppresses ROS production and the expression of MMPs following UVA irradiation[1][2].
AGI-24512 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-24512 blocks growth of MTAP-deleted cancer cells in vitro.
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].
Ac-IHIHIQI-NH2 is a fibril-forming heptapeptide with high catalytic activity to laccase mimics. Ac-IHIHIQI-NH2 exhibits selectivity for hydrophobic p-nitrophenyl (ONp) ester substrates in the process of self-assembly[1][2].
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM)[1][2].
H-Trp-Trp-Trp-OH is a tripeptide consisting of tryptophan. H-Trp-Trp-Trp-OH has antibacterial activity[1].
3’-Azido-3’-deoxy-5-iodouridine 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].
Ginkgolic Acid (C13:0) is a natural anticariogenic agent in that it exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity.IC50 value: Inhibiting the biofilm formation of S. mutans (MBIC (50) = 4 μg/mL); reduced 1-day-developed biofilm of S. mutans by 50 % or more at low concentration (MBRC (50) = 32 μg/mL).Target:In vitro: Ginkgolic Acid (C13:0) inhibited not only the growth of S. mutans planktonic cells at minimum inhibitory concentration (MIC) of 4 μg/mL and minimum bactericidal concentration (MBC) of 8 μg/mL but also the acid production and adherence to saliva-coated hydroxyapatite of S. mutans at sub-MIC concentration. In addition, this agent was effective in inhibiting the biofilm formation of S. mutans (MBIC (50) = 4 μg/mL), and it reduced 1-day-developed biofilm of S. mutans by 50 % or more at low concentration (MBRC (50) = 32 μg/mL). Furthermore Ginkgolic Acid (C13:0) disrupted biofilm integrity effectively [1]. In vivo:
(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor[1]. (R)-Fadrozole also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.[1][2].
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].
CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery[1].
4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid has hypoglycaemic activity. 4-(3-Methyl-5-oxo-2-pyrazolin-1-yl)benzoic acid follows a mechanism based on the response to the oral glucose overcharge[1].
Sutchuenmedin A is a prenylflavonoid. Sutchuenmedin A is isolated from the 70% EtOH extract of Epimedium sutchuenense[1].
BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.
LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line[1].
2-Naphthalen-1,3,4,5,6,7,8-d7-amine is the deuterium labeled 2-Naphthalen-amine[1].
Enokizumab (MEDI-528) is a monoclonal antibody targeting to interleukin (IL)-9. IL-9 regulates the development of airway inflammation, mucus production, airway hyperresponsiveness, and airway fibrosis largely by increasing mast cell numbers and activity in the airways[1].
p-Hydroxyphenethyl anisate is a main constituent of Notopterygium Radix[1].
WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties[1][2].
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor. Ro 41-3290 is an investigational hypnotic.
Thymoctonan (THF-γ2) is the immunomodulatory octapeptide, thymic humoral factor γ2. Thymoctonan has the half-life less than 6 min at 37 °C in blood from human, rat and mouse[1].
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice[1][2].
Thalidomide-5-O-C2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
Macarangioside D, a megastigmane glucoside, possesses radical-scavenging activity[1].
[Ac-Tyr1,D-Phe2]GRF 1-29, amide (human), a growth hormone releasing factor (GRF) analogue, is a vasoactive intestinal peptide (VIP) antagonist[1].
Aloenin (Aloenin A) is a class of anthraquinones isolated from Aloe arborescens. Aloenin has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE)[1][2].