SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase[1][2].
2-Phenylacetamide is an endogenous metabolite.
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects[1]. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones[2].
CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
Hyaluronan synthase is a membrane protein that requires only Mg+2 and two sugar-UDP substrates (GlcUA-UDP and GlcNAc-UDP) to polymerize HA chains. Hyaluronan synthase catalyzes the biosynthesis of hyaluronic acid (HA)[1][2].
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats[1].
MCU-i4 blocks the IP3-dependent mitochondrial Ca2+-uptake, maintaining the gatekeeping role of their target[1][2].
DG5128 is a preferential α2-adrenoceptor antagonist. DG5128 exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.
Glutaric acid induces oxidative stress in brain of young rats.
Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose.
GLP-1R agonist 9 (Compound 96) is a GLP-1R agonist with EC50 values of 1.1 nM and 11 nM against CHO GLP-1R Clone H6 and CHO GLP-1R Clone C6, respectively[1].
SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases[1][2].
Pimelic acid-d4 is the deuterium labeled Pimelic acid[1]. Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
9-PAHPA is a fatty acid esters of hydroxy fatty acid (FAHFA). FAHFAs are a new family of endogenous lipids, have antidiabetic and anti-inflammatory effects[1].
JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity[1].
Pyraclostrobin is a strobilurin fungicide that inhibits mitochondrial complex III of fungal and mammalian cells. Pyraclostrobin induces triglyceride accumulation and triglyceride accumulation in 3T3-L1 cells.
GIP (1-39) (Gastric inhibitory peptide (1-39) (porcine)) is an insulinotropic peptide that stimulats insulin secretion from rat pancreatic islets. GIP (1-39) at 100 nM was able to significantly increase intracellular Ca2+ concentration ([Ca2+]i), and capable of enhancing exocytosis[1].
Allitol is a rare natural polyol that can be used as a sweetener. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS[1].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
Glyurallin A (Compound 79) is isolated from the naturalGlycyrrhiza uralensis. Glyurallin A inhibitsα-Glucosidase(HY-P2802)(IC50=0.3 μM). Glyurallin A can be used in the study of anti-diabetes[1].
Benzylideneacetone is an endogenous metabolite.
STO-609 acetate is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 acetate inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
Transfectam is a cationic lipid able to interact with DNA to form complexes that mediate efficient gene transfer into various eukaryotic cells[1].
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) [1].
(R)-3-Hydroxybutanoic acid-d3 ((R)-(-)-3-Hydroxybutanoic acid-d3) sodium is a deuterated labeled (R)-3-Hydroxybutanoic acid sodium. (R)-3-Hydroxybutanoic acid sodium is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones[1][2].
Foenumoside B is a triterpene saponin isolated from Lysimachia foenum-graecum. Foenumoside B activates AMPK signaling, inhibits PPARγ-induced adipogenesis, and shifts lipid metabolism toward lipolysis. Foenumoside B can be used in the study of obesity and obesity-related metabolic diseases[1].
L-Glutamine is a non-essential amino acid present abundantly throughout the body and is involved in gastrointestinal disorders.Target: mGluRGlutamine (abbreviated as Gln or Q) is one of the 20 amino acids encoded by the standard genetic code. It is not recognized as an essential amino acid, but may become conditionally essential in certain situations, including intensive athletic training or certain gastrointestinal disorders. Its side-chain is an amide formed by replacing the side-chain hydroxyl of glutamic acid with an amine functional group, making it the amide of glutamic acid. Its codons are CAA and CAG. In human blood, glutamine is the most abundant free amino acid, with a concentration of about 500-900 μmol/L. Glutamine is synthesized by the enzyme glutamine synthetase from glutamate and ammonia. The most relevant glutamine-producing tissue is the muscle mass, accounting for about 90% of all glutamine synthesized. Glutamine is also released, in small amounts, by the lung and the brain. Although the liver is capable of relevant glutamine synthesis, its role in glutamine metabolism is more regulatory than producing, since the liver takes up large amounts of glutamine derived from the gut. The most eager consumers of glutamine are the cells of intestines, the kidney cells for the acid-base balance, activated immune cells, and manycancer cells. In respect to the last point mentioned, different glutamine analogues, such as DON, Azaserine or Acivicin, are tested as anticancer drugs.
Potent, allosteric GPR55 antagonist
Lumirubin, a structural isomer of bilirubin, is the main photooxidative product formed during phototherapy for the treatment of neonatal jaundice, and has a certain pro-inflammatory effect[1].
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8±0.2 nM.