mitogenesis

SU5205 is a VEGFR2 inhibitor.

Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG) that is tightly attached to cell surface or extracellular matrix proteins.

EHNA hydrochloride is a selective inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) and adenosine deaminase (ADA) with anticancer activity, increasing intracellular adenosine concentration in a treatment time-dependent manner. EHNA hydrochloride inhibits PHA and NaI04 mitogenesis.

AG 370, an indole tyrphostin, is a potent inhibitor of PDGF-induced mitogenesis with an IC50 of 20 μM, and it shows weak inhibition of the EGF receptor.

NGB 2904 is a potent and selective antagonist of dopamine D3 receptor (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes mitogenesis stimulated by quinpirole (IC50 = 6.8 nM).

Arachidonic acid is metabolized in the vascular endothelium to epoxytrienoic acids (EETs or EpETrEs) by cytochrome P450 enzymes. The EETs are released in response to acetylcholine, bradykinin, arachidonic acid, or cyclic stretch. (±)14(15)-EET-SI is the methyl sulfonamide analog of 14(15)-EET. This substitution results in a metabolically more stable compound because it is not sensitive to β-oxidation or membrane esterification. (±)14(15)-EET-SI is equipotent to 14(15)-EET in vascular agonist activity as measured by relaxation of precontracted bovine coronary arteries. In addition, 14(15)-EET and the methyl sulfonamide analog both stimulate tyrosine phosphorylation and induce mitogenesis in renal epithelial cells.

PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2).

Phosphatidylinositols, comprising about 10% of total cellular phospholipids, are glycerophospholipids featuring a glycerol backbone, two non-polar fatty acid tails (primarily C16:0 and C18:0), and a polar inositol head group. Synthesized from cytidine diphosphate diacylglycerol (CPD-DAG) and myoinositol via phosphoinositol synthase, these compounds play pivotal roles in cellular processes, including calcium regulation, vesicle trafficking, mitogenesis, cell survival, and actin rearrangement. Phosphorylation of their inositol rings produces phosphoinositides, crucial for these cellular functions. [Matreya, LLC. Catalog No. 1048]

Mammalian bombesin-like peptide neurotransmitter that is an agonist for the gastrin-releasing peptide receptor (GRPR). GRP has been reported to activate GABAergic interneurons in the amygdala leading to increased GABA release and fear suppression in mice

Lipopolysaccharides, from E. coli (Escherichia coli) K-235, are endotoxins derived from Escherichia coli and serve as TLR-4 activators. They are an S-type LPS capable of activating pathogen-associated molecular patterns (PAMP) of the immune system and inducing the secretion of exosomes. This compound is characterized by a typical three-part structure comprising the O-antigen, core oligosaccharide, and Lipid A. Additionally, lipopolysaccharides from E. coli K-235 stimulate mitogenesis in C57BL/10ScN spleen cells and, when purified by butanol and deoxycholate methods, can stimulate spleen cells from C57BL/10ScCR and C3H/HeJ mice.