endothelial

INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor that disrupts CN-NFAT signaling by targeting the NFAT(P) substrate at the calcineurin (CN) phosphatase site.

Azilsartan (TAK-536) is an Angiotensin 2 Receptor Blocker that acts as an Angiotensin 2 Type 1 Receptor Antagonist, leading to a physiologic effect of decreased blood pressure.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

Valsartan (CGP 48933) is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension.

SU5205 is a VEGFR2 inhibitor.

Cinanserin hydrochloride (SQ 10643), a high-affinity antagonist of the 5-HT2 receptor (Ki: 41 nM), is also a 3C-like protease inhibitor of severe acute respiratory syndrome coronavirus.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.

BMS309403 is a potent and selective inhibitor of adipocyte fatty acid binding protein aFABP. It improves endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells. It interacts with the fatty acid binding pocket inside the protein and competitively inhibits the binding of endogenous fatty acids.

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.

MYLS22 is a first-in-class and selective inhibitor of optic atrophy 1 (OPA1) . MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression. It with anti-angiogenesis and anti-cancer activity.

Copper tripeptide (GHK-Cu) is a naturally occurring copper complex of the tripeptide glycyl-L-histidyl-L-lysine, with a strong affinity for copper(II). First isolated from human plasma, it is also found in saliva and urine.

Anti-Mouse Pan-endothelial Cell Antigen/MECA-32 Antibody (MECA-32) is an IgG2a, κ antibody inhibitor derived from rats, targeting the mouse Pan-endothelial Cell Antigen/MECA-32.

Endothelial lipase inhibitor-1 is a potent inhibitor of endothelial lipase with an IC50 of 49 nM.

Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell (Ac-Pro-Tyr-Asn-Ser-Ser-Pro-Arg-Pro-Glu-Gln-His-Lys-Ser-Tyr-Lys-Cys) is a peptide that inhibits the function of NOSs as a result it blocks the production of NO. Because of the invol

Bovine Endothelial cell growth supplement is a medium additive that acts as an endothelial cell growth supplement (ECGS), enhancing the proliferation of human saphenous vein endothelial cells (HSVEC) and human umbilical vein endothelial cells (HUVEC).

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

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.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRβ, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.