Angiogenesis inhibitor 3

Angiogenesis Inhibitor 3 (Compound 8) is a potent substance that effectively inhibits the growth of HUVEC and HCT-15 cells, demonstrating IC50 values of 1.00 and 0.71 μM, respectively. It not only induces apoptosis in these cells but also exhibits significant anticancer activity by suppressing cancer cell invasion. Furthermore, this compound successfully inhibits angiogenesis in zebrafish embryos [1].

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

Batimastat (BB94) (BB-94) is an effective, broad-spectrum matrix metalloprotease (MMP) inhibitor. Batimastat induces extracellular matrix degradation and inhibits angiogenesis, tumor growth and invasion, and metastasis.

NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity) commonly used in nitric oxide signaling pathway research. It inhibits sGC activity in mouse cerebellum homogenates and neuronal NO synthase (IC50: 17 nM and 20 nM), inhibits 3-morpholino-sydnonimine (SIN-1)-elicited cyclic GMP formation in human cultured umbilical vein endothelial cells (IC50: 30 nM), and completely inhibits NO-dependent relaxant responses in non-vascular smooth muscle (1 μM). NS-2028 also decreases vascular endothelial growth factor-induced angiogenesis and permeability.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1 3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

Motesanib (AMG 706) is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

LOX-IN-3, an orally active inhibitor of lysyl oxidase (LOX), holds potential application in the fields of fibrosis, cancer, and angiogenesis research[1].

Tinengotinib is a multikinase inhibitor targeting a series of kinases involved in cancer cell proliferation, angiogenesis, and regulation of immune response, including Aurora kinase A B, Janus kinase (JAK1 2), fibroblast growth factor receptor (FGFR1 2 3), vascular endothelial growth factor receptors (VEGFRs), and other tyrosine kinases. Tinengotinib has shown good tolerability and preliminary efficacy in clinical trials in a variety of advanced solid tumors.

Su1498 (Tyrphostin SU 1498) is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), having negligible activity at several other serine threonine and tyrosine kinases.1, 2 It effectively blocks signaling through VEGFR2 both in vitro and in vivo.1, 3 SU 1498 is used to study the role of VEGFR2 signaling in diverse processes, including angiogenesis, tumor growth, neural progenitor cell survival, and neuroregeneration.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

LOX-IN-3 dihydrochloride monohydrate (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor, intended for research in fibrosis, cancer, and angiogenesis [1].

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.

EVT801 is a highly selective and low-toxic VEGFR-3 inhibitor that inhibits VEGF-C-induced tumor lymphoid and angiogenesis and reduces important circulating immunosuppressive factors (CCL4, CCL5) and myeloid-derived suppressor cells (MDSC).

TIE-2 VEGFR-2 kinase-IN-3, a benzimidazole derivative, is a potent inhibitor of tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

Sutetinib is an orally effective tyrosine kinase inhibitor that targets enzymes linked to tumor growth and angiogenesis, such as VEGFR (VEGFR-1 2 3 with Ki= 0.009 µM), PDGFR (PDGFR-α β with Ki= 0.008 µM), and the proto-oncogene cKIT. It inhibits the proliferation, migration, and tubular structure formation of endothelial and fibroblast cells, demonstrating antitumor activity across various cancer cell lines.

Sutetinib maleate is the maleate salt form of Sutetinib. This compound functions as an orally effective tyrosine kinase (tyrosine kinase) inhibitor that targets tyrosine kinases associated with tumor growth and angiogenesis, including VEGFR (VEGFR-1 2 3 with Ki=0.009 µM), PDGFR (PDGFR-α β with Ki=0.008 µM), and the proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial and fibroblast cells, displaying antitumor activity across various tumor cell lines.

Rhamnazin (3',7-Dimethylquercetin) is an orally active VEGFR2 signaling inhibitor with anti-angiogenesis, anti-tumor, antioxidant, and anti-inflammatory activities. It inhibits VEGFR2 kinase and is used for leukemia research.