1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. VEGFR

VEGFR

Vascular endothelial growth factor receptor

VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3). Each receptor has seven immunoglobulinlike domains in the extracellular domain, a single transmembrane region, and a consensus tyrosine kinase sequence interrupted by a kinase insert domain. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. The VEGF family members VEGF-A, -B, -C, -D, -E, and PlGF, and the human immunodeficiency (HIV) Tat protein bind in specific patterns to three related receptor protein tyrosine kinases, VEGFR1, 2, and 3, and induce the formation of homo- and heteromeric receptor complexes. Binding of VEGF to VEGFR causes dimerization and autophosphorylation of the receptor. Intracellular proteins such as VEGFR-associated protein (VRAP), PLC, and Sck that associate with specific tyrosine residues of VEGFR are phosphorylated upon receptor activation. Several signal transduction pathways are activated by the binding of VEGF to its receptor, leading to increased proliferation, survival, permeability, and migration of cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15992
    BIBF 1202
    Inhibitor 99.82%
    BIBF 1202 is the carboxylate metabolite of Nintedanib (HY-50904) which inhibits VEGFR2 kinase with an IC50 of 62 nM.
    BIBF 1202
  • HY-173496
    ST6GAL1-IN-1
    Inhibitor 99.22%
    ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC50 = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC).
    ST6GAL1-IN-1
  • HY-101259
    BMS-195614
    Inhibitor 99.5%
    BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis.
    BMS-195614
  • HY-13718
    Oglufanide
    Inhibitor 98.93%
    Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. Oglufanide inhibits vascular endothelial growth factor (VEGF). Oglufanide can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide shows antitumor and anti-angiogenesis activities.
    Oglufanide
  • HY-103002
    SU5408
    Inhibitor 98.0%
    SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
    SU5408
  • HY-P3226
    JB-1
    Activator 99.63%
    JB-1, an IGF-I analog, is a selective IGF-I receptor inhibitor that does not interact with IGF-II. JB-1 competes with IGF-I for binding to IGF-1R and blocks receptor autophosphorylation. JB-1 increases the level of sVEGFR-1. JB-1 normalizes retinal abnormalities, including reducing retinal neovascularization. JB-1 is applicable to studies related to oxygen-induced retinopathy.
    JB-1
  • HY-100419
    BFH772
    Inhibitor
    BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.
    BFH772
  • HY-N0442
    5-O-Methylvisammioside
    Inhibitor 99.90%
    5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.
    5-O-Methylvisammioside
  • HY-B1076
    Medrysone
    Activator 99.79%
    Medrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury.
    Medrysone
  • HY-144707
    AK-778-XXMU
    Inhibitor 99.96%
    AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and exhibits significant cancer-suppressing potency. AK-778-XXMU inhibits the ID2-KDR signaling axis, thereby down-regulating the downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and up-regulating the tumor suppressor factor (PTEN). AK-778-XXMU can be used for the study of glioma.
    AK-778-XXMU
  • HY-10201R
    Sorafenib (Standard)
    Inhibitor
    Sorafenib (Standard) is the analytical standard of Sorafenib. This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib (Standard)
  • HY-13302
    CP-547632
    Inhibitor 99.94%
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
    CP-547632
  • HY-103647
    K00546
    Inhibitor 99.48%
    K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively.
    K00546
  • HY-P10831
    GNQWFI
    Antagonist 99.45%
    GNQWFI, an anti-Flt1 peptide, is a VEGFR1-specific antagonist. GNQWFI blocks the interaction of VEGFR1 with various VEGFR1 ligands, such as VEGFA, VEGFB, and placental growth factor (PIGF) and inhibits VEGF-induced endothelial cell migration and tube formation. GNQWFI is promising for research of cancer, asthma, and other ocular diseases.
    GNQWFI
  • HY-10337
    Brivanib
    Inhibitor 99.92%
    Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
    Brivanib
  • HY-112292A
    GW806742X hydrochloride
    Inhibitor 98.30%
    GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
    GW806742X hydrochloride
  • HY-P9973
    Brolucizumab
    Inhibitor 99.90%
    Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). Brolucizumab can be used for the research of cancer.
    Brolucizumab
  • HY-P1663
    ATWLPPR Peptide
    Inhibitor 99.63%
    ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
    ATWLPPR Peptide
  • HY-N0419
    Quercimeritrin
    Ligand 99.48%
    Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer.
    Quercimeritrin
  • HY-16265
    JI-101
    Inhibitor 98.99%
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
    JI-101
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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