platelet factor 4

Platelet Factor 4 (58-70), human, is a polypeptide comprising the 58-70 amino acid sequence of Platelet Factor 4 (PF-4) residues.

Platelet factor 4 (59-70) elicits human neutrophil & monocyte chemotaxis.

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.

AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4].

Benafentrine dimaleate is a platelet activating factor receptor (PAFR) antagonists and phosphodiesterase (PDE) 3/4 inhibitors.

JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).

Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a concentration of 100 μM.3 Dietary administration of collinin (0.05% w/w) reduces the number of mice with tumors and the number of tumors per mouse in a mouse model of colitis-related carcinogenesis.4 |1. Kim, S., Seo, H., Al Mahmud, H., et al. In vitro activity of collinin isolated from the leaves of Zanthoxylum schinifolium against multidrug- and extensively drug-resistant Mycobacterium tuberculosis. Phytomedicine 46, 104-110 (2018).|2. Nguyen, P.-H., Zhao, B.T., Kim, O., et al. Anti-inflammatory terpenylated coumarins from the leaves of Zanthoxylum schinifolium with α-glucosidase inhibitory activity. J. Nat. Med. 70(2), 276-281 (2016).|3. I.S., C., Lin, Y.C., Tsai, I.L., et al. Coumarins and anti-platelet aggregation constituents from Zanthoxylum schinifolium. Phytochemistry 39(5), 1091-1097 (1995).|4. Kohno, H., Suzuki, R., Curini, M., et al. Dietary administration with prenyloxycoumarins, auraptene and collinin, inhibits colitis-related colon carcinogenesis in mice. Int. J. Cancer 118(12), 2936-2942 (2006).

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

Lp-PLA2-IN-4 is a potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor and an inhibitor of platelet-activating factor acetylhydrolase (PAF-AH), a phospholipase A2 involved in lipoprotein lipid or phospholipid hydrolysis. Lp-PLA2-IN-4 has potential for study in diseases associated with Lp-PLA2 activity, such as Alzheimer's disease and atherosclerosis. [Compound 38]

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg/kg/day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima/media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

Pinocembrin 7-O-[4",6"-(S)-HHDP]-β-D-glucoside, is a complex polyphenol compound that has been shown to exhibit modest antiproliferative effects in platelet-derived growth factor (PDGF)-induced HSC-T6 hepatic stellate cells with an IC50 of 200 μM. further experiments confirm that Pinocembrin 7-O-[4",6"-(S)-HHDP]-β-D-glucoside possesses a more remarkable anti-proliferative effect specifically against activated hepatic stellate cells (HSCs), which are key drivers of liver fibrosis.

P4pal10 TFA, the TFA salt form of P4pal10, serves as an antagonist of the protease-activated receptor 4 (PAR4). This compound inhibits platelet aggregation and thrombin generation induced by tissue factor (TF), exhibiting anticoagulant and antithrombotic activities. Additionally, P4pal10 TFA alleviates carrageenan-induced edema and neutrophil infiltration, and ameliorates damage in rat myocardial ischemia/reperfusion (I/R) models.