differentiated

Glufosinate ammonium is a phosphinic acid analog of glutamic acid and an herbicide with neurotoxic activity. It is converted by plant cells into PT (L-phosphinothricin).

CHPG is a selective mGluR5 agonist that reduces LDH release and neuronal apoptosis, activates the ERK and Akt pathways, and protects against traumatic brain injury. It also increases the number of differentiated human OPCs and alleviates LPS-induced inflammation.

Verlukast is an (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide diffe

YK-2168 is a differentiated selective inhibitor of CDK9.

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay. [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample - Signallow)/(Signalhigh - Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.

Protein conjugates in tissue regeneration 2 (PCTR2) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is converted to PCTR1 by glutathione S-transferase and to PCTR2 via γ-glutamyl transpeptidase. PCTR2 is found in resolving mouse exudate and in both M1 and M2 macrophages differentiated from isolated human monocytes.

Protein conjugates in tissue regeneration 3 (PCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is converted to PCTR1 by glutathione S-transferase and to PCTR2 and PCTR3 via peptidases. PCTR3 is found in infected mouse spleens and resolving exudate as well as isolated human spleen and septic plasma. It is also found in both M1 and M2 macrophages differentiated from isolated human monocytes.

CAY10781 is an inhibitor of the protein-protein interaction between neuropilin-1 (NRP-1) and VEGF-A.1It inhibits the interaction by 43% when used at a concentration of 12.5 μM. CAY10781 also inhibits VEGF-A-induced phosphorylation of VEGFR2 in catecholamine A-differentiated (CAD) cells when used at the same concentration. 1.Perez-Miller, S., Patek, M., Moutal, A., et al.In silico identification and validation of inhibitors of the interaction between neuropilin receptor 1 and SARS-CoV-2 Spike proteinbioRxiv308783(2020)

DOTATATE acetate is a DOTA-binding peptide, a growth inhibitor analog, and a novel PET tracer involved in the assessment of functional imaging of highly differentiated neuroendocrine tumors (NETs).

IMP2-IN-1 (compound 4) is an effective IMP2 inhibitor with an IC50 of 81.3-127.5 μM for IMP2 RNA, reducing IMP2 levels in SW480 cells and significantly inhibiting the activity of both differentiated and undifferentiated Huh7 cells.

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

NSC-18725 is a novel inhibitor of growth of intracellular Mycobacterium tuberculosis, inducing autophagy in differentiated THP-1 macrophages.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg ml. Gliclazide (5 mg kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

Lemzoparlimab (TJ011133) is a differentiated anti-CD47 humanized antibody with anti-tumor activity, used in the study of myeloid leukemia.

BDS-I, a marine toxin derived from Anemonia sulcata, functions as a selective inhibitor of the potassium channel, specifically targeting Kv3.4. It impedes the Aβ1-42-induced augmentation of Kv3.4 activity, caspase-3 activation, and distortion of nuclear morphology in NGF-differentiated PC-12 cells. Moreover, BDS-I effectively counteracts the cell death induced by the Aβ peptide [1].

Gangliotetraose (Gg4), a tetrasccharide, predominantly comprises GM1 and its sialylated derivatives, which play a crucial role in modulating nuclear Ca2+ efflux and maintaining lower nuclear Ca2+ levels in differentiated neurons. Moreover, GM1 influences neuronal plasticity, repair mechanisms, and neurotrophin release in the brain [1] [2].

Gastric inhibitory peptide (GIP) (22-51), a pro-atherogenic peptide comprised of 30 amino acids from the residues 22-51 of its precursor protein proGIP, is present in human plasma. It activates the degradation of IκB-α and the nuclear translocation of NF-κB in both macrophage-differentiated THP-1 cells and human aortic endothelial cells at a concentration of 1 µM. Additionally, in ApoE-/- mice, GIP (22-51) escalates the area of atherosclerotic lesions and plaque development in vivo.

5β,6β-Epoxycholestanol is an oxidative metabolite of cholesterol produced through radical and non-radical oxidation at the 5,6-double bond. It induces the release of lactate dehydrogenase (LDH) and apoptosis in differentiated macrophage U937 cells. This compound has been identified in human fatty streaks and advanced atherosclerotic lesions but is absent in normal aortic tissue.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside) is a flavonol from Morettia philaena that inhibits α-amylase, α-glucosidase, and acetylcholinesterase. It exhibits neuroprotective activity, slowing amyloid β peptide-induced damage in differentiated neuronal cells SH-SY5Y, and can be used in the study of neurological disorders such as Alzheimer's disease.

Selaginellin has a neuroprotective effect against L-glutamate-induced neurotoxicity through mechanisms related to anti-oxidation and anti-apoptosis via scavenging reactive oxygen species and up-regulating the expression of klotho gene. Selaginellin shows