Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent CXCR4 antagonist and an anti-angiogenic drug that is of potential value in treating choroid neovascularization.
Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1 Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1 2 and Akt.
CGC 11093 is a polyamine analog; inhibits growth of human prostate tumor xenografts in nude mice. It may prove useful in promoting regression of choroidal neovascularization.
Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1
Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.
(±)11(12)-EET is a fully racemic version of the R S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in the renal cortical collecting duct when used at a concentration of 100 nM.[5]11(12)-EET (50 μg kg per day) increases adhesion of isolated peripheral blood leukocytes in a chamber coated with P-selectin and ICAM-1 but does not affect choroidal neovascularization size following laser photocoagulation[6] It also has anti-inflammatory, angiogenic, and cardioprotective properties[7]
ABT-510 is synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).