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-N0563
    Alizarin
    Activator 99.48%
    Alizarin is a natural dye. Alizarin can be extracted from the roots of madder plant. Alizarin activates AMPK and VEGFR2/eNOS pathway. Alizarin regulates PI3K/Akt and inhibits NF-κB pathway. Alizarin enhances CYP1A1 enzyme activity. Alizarin has protective effects on hypertension and vascular endothelial dysfunction. Alizarin has anti-tumor activity against multiple cancers including pancreatic cancer, breast cancer, osteosarcoma and liver cancer. Alizarin has been widely used as a pigment in textile fabrics and paintings.
    Alizarin
  • HY-112292A
    GW806742X hydrochloride
    Inhibitor 98.77%
    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-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-Y0121
    Ethyl cinnamate
    Inhibitor 99.80%
    Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta.
    Ethyl cinnamate
  • HY-10408
    Ki20227
    Inhibitor 99.51%
    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.
    Ki20227
  • HY-100349
    SU4312
    Inhibitor 99.74%
    SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
    SU4312
  • HY-119367
    ODM-203
    Inhibitor 99.62%
    ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.
    ODM-203
  • HY-12018
    Vatalanib dihydrochloride
    Inhibitor 99.68%
    Vatalanib dihydrochloride (PTK787 dihydrochloride) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
    Vatalanib dihydrochloride
  • HY-10977A
    Tivozanib hydrochloride hydrate
    Inhibitor 99.83%
    Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy.
    Tivozanib hydrochloride hydrate
  • HY-15506
    TAK-593
    Inhibitor 99.66%
    TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
    TAK-593
  • 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-16018A
    Ilorasertib hydrochloride
    Inhibitor 98.48%
    Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
    Ilorasertib hydrochloride
  • HY-10497
    BMS-794833
    Inhibitor 99.52%
    BMS-794833 is a VEGFR2 and Met inhibitor extracted from patent WO2009094417, compound example 1; has IC50s of 15 and 1.7 nM, respectively.
    BMS-794833
  • HY-P99215
    Parsatuzumab
    Modulator
    Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition.
    Parsatuzumab
  • HY-B2082
    Fursultiamine
    Inhibitor 99.92%
    Fursultiamine is a vitamin B1 derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B1?deficiency, osteoarthritis (OA) and cancer research.
    Fursultiamine
  • HY-N2575
    Hypocrellin A
    Inhibitor 99.73%
    Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml).
    Hypocrellin A
  • HY-15992
    BIBF 1202
    Inhibitor 99.82%
    BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
    BIBF 1202
  • HY-10204
    OSI-930
    Inhibitor 98.33%
    OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα, Flt-3 and Abl. OSI-930 has antitumor activity.
    OSI-930
  • HY-160259
    VEGFR-2-IN-39
    Inhibitor 99.85%
    VEGFR-2-IN-39 (PROTAC-5) is a PROTAC targeting VEGFR-2 (IC50: 208.6 nM). VEGFR-2-IN-39 has low toxicity.VEGFR-2-IN-39 inhibits the proliferation of EA.hy926, one of HUVECs, in a concentration-dependent manner, with an IC50 of 38.65 µM.
    VEGFR-2-IN-39
  • HY-126437
    Poly-L-lysine hydrobromide (MW 30000-70000)
    Inhibitor
    Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material.
    Poly-L-lysine hydrobromide (MW 30000-70000)
Cat. No. Product Name / Synonyms Species Source
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