VEGFR Inhibitor

VEGFR2-IN-4 (compound 25) is a potent and selective VEGFR2 kinase inhibitor, with a GI₅₀ of 0.7 nM. VEGFR2-IN-4 shows anti-angiogenic effect. VEGFR2-IN-4 can be used for the research of rheumatoid arthritis.

Motesanib (Standard) is the analytical standard of Motesanib. This product is intended for research and analytical applications. Motesanib (AMG 706) is a potent ATP-competitive inhibitor of?VEGFR1/2/3?with?IC50s?of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.

Ki20227 (Standard) is the analytical standard of Ki20227 (HY-10408). This product is intended for research and analytical applications. Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC₅₀s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.

PD173074 (Standard) is the analytical standard of PD173074. This product is intended for research and analytical applications. PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.

SU14813 (Standard) is the analytical standard of SU14813 (HY-10501). This product is intended for research and analytical applications. SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.

Naphazoline (hydrochloride) (Standard) is the analytical standard of Naphazoline (hydrochloride). This product is intended for research and analytical applications. Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.

Thymoquinone (Standard) is the analytical standard of Thymoquinone. This product is intended for research and analytical applications. Thymoquinone is an orally active natural product isolated from N. sativa Thymoquinone down-regulates the VEGFR2-PI3K-Akt pathway. Thymoquinone has antioxidant, anti-inflammatory, anticancer, antiviral, anticonvulsant, antifungal, antiviral, antiangiogenic activity and hepatoprotective effects. Thymoquinone can be used to study Alzheimer's disease, cancer, cardiovascular disease, infectious disease and inflammation .

Liensinine (Standard) is the analytical standard of Liensinine (HY-N0484). This product is intended for research and analytical applications. Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.

Azaspirene ((-)-Azaspirene) is an angiogenesis and Raf-1 activation inhibitor isolated from the fungus Neosartorya sp. Azaspirene inhibits vascular endothelial growth factor (VEGF)-induced human umbilical vein endothelial cell (HUVEC) migration and Raf-1 activation, but has no effect on the activation of kinase insert domain-containing receptor/fetal liver kinase 1 (VEGF receptor 2).

DMBT is an orally effective anti-tumor metastasis and anti-angiogenesis agent. DMBT downregulates key molecules such as EGFR/p-Akt/HIF-1α/VEGF/MMP-9, inhibits the HIF-1α/VE-cadherin (cadherin)/MMPs and Nrf2/HO-1 signaling pathways, and reduces hypoxia-induced ROS levels as well as the secretion and activity of MMP-9. DMBT inhibits hypoxia-induced vasculogenic mimicry, cancer cell migration, invasion and metastasis, and exhibits no obvious cytotoxicity to normal cells. DMBT reduces the area of laser-induced choroidal neovascularization lesions. DMBT can be used in studies related to breast cancer, melanoma and macular degeneration.

Bucillamine (Standard) is the analytical standard of Bucillamine. This product is intended for research and analytical applications. Bucillamine (SA96) is an orally active and potent sulfhydryl donor and antioxidant. Bucillamine is also an antirheumatic agent with antiangiogenic properties. Bucillamine can protect against Ischemia/reperfusion (I/R) injury in high-risk organ transplants. Bucillamine inhibits the production of VEGF. Bucillamine can be used for the research of choroidal neovascularization (CNV) and rheumatoid arthritis (RA).

VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC₅₀ of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI₅₀=1.6 µM). VEGFR-2-IN-12 has antitumor activity.

VEGFR-2-IN-9 (KDR-in-4) is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC₅₀ of 7 nM.