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-P10580
    Vasculotide
    Activator 99.84%
    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-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-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-118105
    RK-20448
    Inhibitor 99.38%
    RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 (HY-15764).
    RK-20448
  • 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 VEGFR1/2/3, 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
  • 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 VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate (Standard)
  • HY-P991663
    AMG-780
    Inhibitor
    AMG-780 is a fully human IgG2 antibody that targets angiopoietin 1 (Ang1) (IC50 = 4.5 nM) and angiopoietin 2 (Ang2) (IC50 = 0.06 nM). AMG-780 inhibits tumor growth in the Colo205 xenograft mouse model by inhibiting both Ang1 and Ang2. AMG-780 is indicated for the research of cancers such as colon cancer.
    AMG-780
  • 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-E70783
    TIE2 Y1108F Recombinant Human Active Protein Kinase
    TIE2 plays an important role in vascular formation and maintenance. Mutations in TIE2 lead to vascular malformations, which are painful vascular lesions that cause disfigurement, bleeding, and thrombosis. TIE2 Y1108F is the most mutation of TIE2. TIE2 Y1108F Recombinant Human Active Protein Kinase is a recombinant TIE2 Y1108F protein that can be used to study TIE2 Y1108F-related functions.
    TIE2 Y1108F Recombinant Human Active Protein Kinase
  • HY-P991385
    UBX2050
    Inhibitor
    UBX2050 is a human monoclonal antibody (mAb) targeting TIE2. UBX2050 can be used in Age-related macular degeneration, Diabetic macular oedema and Diabetic retinopathy research.
    UBX2050
  • HY-156635
    TIE-2/VEGFR-2 kinase-IN-3
    Inhibitor
    TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-3
  • HY-156637
    TIE-2/VEGFR-2 kinase-IN-4
    Inhibitor
    TIE-2/VEGFR-2 kinase-IN-4, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 5.2 nM and 5.1 nM, respectively. TIE-2/VEGFR-2 kinase-IN-4 can be used for the research of angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-4
  • HY-N3634
    Corylifol C
    Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively.
    Corylifol C
  • HY-P991384
    DX-2240
    Inhibitor
    DX-2240 is a human monoclonal antibody (mAb) targeting TIE1. DX-2240 inhibits tumor growth and sensitizes tumor vasculature to anti-angiogenic agents (VEGF pathway inhibitors).
    DX-2240
  • HY-16782R
    Pexmetinib (Standard)
    Inhibitor
    Pexmetinib (Standard) is the analytical standard of Pexmetinib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-164529
    SJ-C1044
    Inhibitor
    SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.
    SJ-C1044
  • HY-10331R
    Regorafenib (Standard)
    Inhibitor
    Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. 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 VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib (Standard)
  • HY-14243
    CEP-14083
    Inhibitor
    CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma.
    CEP-14083
Cat. No. Product Name / Synonyms Application Reactivity

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