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

Tie

Angiopoietin receptor

Angiopoietins (Angs) are important vascular growth factors that regulate vascular remodeling, maturation, and stabilization. Angs also regulate vascular reactivity through regulating the production of nitric oxide (NO). The Angs family includes Ang1, Ang2, and Ang4 (a human orthologue of mouse Ang3) which interacts with tyrosine kinase receptors (Tie1 and Tie2). The angiopoietins receptors Tie1 and Tie2 (also known as TEK) are almost exclusively expressed in the endothelium, but there is some expression also in haematopoietic cells. The growth factors Ang1, Ang2 and Ang4 (the human orthologue of mouse Ang3) are ligands for Tie2, whereas Tie1 is an orphan receptor that can nevertheless be activated by angiopoietins via its interaction with Tie2. Ang-Tie signaling is involved in various processes of vascular development and remodeling in different diseases.

Tie Isoform Specific Products:

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10331
    Regorafenib
    Inhibitor 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib
  • HY-109041
    Razuprotafib
    Activator ≥98.0%
    Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).
    Razuprotafib
  • HY-10331A
    Regorafenib monohydrate
    Inhibitor 99.96%
    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate
  • HY-100556
    Tie2 kinase inhibitor 1
    Inhibitor 99.90%
    Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
    Tie2 kinase inhibitor 1
  • HY-16782
    Pexmetinib
    Inhibitor 99.81%
    Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
    Pexmetinib
  • HY-P10580
    Vasculotide
    Activator
    Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock.
    Vasculotide
  • HY-10331AR
    Regorafenib monohydrate (Standard)
    Inhibitor
    Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate (Standard)
  • HY-160708
    Tie2 kinase inhibitor 3
    Inhibitor
    Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis.
    Tie2 kinase inhibitor 3
  • HY-108333
    SB-633825
    Inhibitor 98.52%
    SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.
    SB-633825
  • HY-100756
    BAY-826
    Inhibitor 99.94%
    BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.
    BAY-826
  • HY-P99330
    Vanucizumab
    Inhibitor
    Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects.
    Vanucizumab
  • HY-100394
    NVP-BAW2881
    Inhibitor 98.54%
    NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2/KDR/Flk-1 inhibitor with an IC50 of 4 nM.
    NVP-BAW2881
  • HY-12572
    TIE-2/VEGFR-2 kinase-IN-2
    Inhibitor 99.79%
    TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2/KDR/Flk-1 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.
    TIE-2/VEGFR-2 kinase-IN-2
  • HY-112423
    CE-245677
    Inhibitor 98.14%
    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
    CE-245677
  • HY-125741
    GW768505A free base
    Inhibitor 98.66%
    GW768505A free base is a potent dual inhibitor of VEGFR2/KDR/Flk-1 (VEGFR2/KDR/Flk-1) and Tie-2, with a pIC50 of 7.81 for VEGFR2/KDR/Flk-1. GW768505A free base has anti-angiogenic activity。
    GW768505A free base
  • HY-P99510
    Zansecimab
    Inhibitor
    Zansecimab (LY-3127804) is an immunoglobulin G4-kappa, a monoclonal antibody against angiopoietin 2 (Ang 2). Zansecimab has potential applications in angiogenesis and immune regulation.
    Zansecimab
  • HY-112294
    TIE-2/VEGFR-2 kinase-IN-1
    Inhibitor 99.91%
    TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-1
  • HY-10331B
    Regorafenib mesylate
    Inhibitor
    Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.
    Regorafenib mesylate
  • HY-112475
    Flt-3 Inhibitor III
    Inhibitor
    Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects.
    Flt-3 Inhibitor III
  • HY-156638
    TIE-2/VEGFR-2 kinase-IN-5
    Inhibitor
    TIE-2/VEGFR-2 kinase-IN-5 is an anti-angiogenic agent. TIE-2/VEGFR-2 kinase-IN-5 also is a potent TIE-2 and VEGFR-2 tyrosine kinase inhibitor with pIC50 values of 7.78 nM and 8.11 nM, respectively. TIE-2/VEGFR-2 kinase-IN-5 can be used for the research of angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-5
Cat. No. Product Name / Synonyms Application Reactivity

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