2. Signaling Pathways
  3. Cytoskeleton
  4. Integrin
  5. αvβ3 Isoform

αvβ3

Integrin αvβ3 is a heterodimeric receptor that mediates cell adhesion to extracellular matrix (ECM) proteins, primarily vitronectin, and regulates angiogenesis and tumor cell survival[1][2]. Mechanistically, αvβ3 interacts with intracellular signaling pathways including FAK/ERK to promote osteogenesis and endothelial migration, making it a pivotal regulator of tissue remodeling and pathological angiogenesis[3]. In disease models, αvβ3 expression is elevated in neuroendocrine prostate cancer, medulloblastoma, glioblastoma, and ovarian carcinoma, correlating with tumor aggressiveness, metastatic potential, and radioresistance[4][5][6][7]. Compared with related αv integrins such as αvβ5 and αvβ6, αvβ3 exhibits higher expression in tumor-associated vasculature and metastatic tumor cells, and it mediates platelet-assisted extravasation during hematogenous metastasis[8][2]. In experimental applications, selective αvβ3 inhibitors and agonists, including cyclic RGD peptides and fluorescent or radiolabeled RGD-based ligands, have been used to modulate angiogenesis, visualize tumors via PET/SPECT imaging, and inhibit ectopic ossification or tumor progression in preclinical models[3][6][7][9]. The combination of αvβ3-targeted imaging and pharmacologic blockade provides a dual platform for both mechanistic studies and potential therapeutic intervention in oncology and vascular disease research[6][9].

References:

Cat. No. Product Name Effect Purity
  • HY-16141
    Cilengitide
    		Antagonist 99.91%
    Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.
  • HY-P0023
    Cyclo(-RGDfK)
    		Inhibitor 99.83%
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-P2300
    Cyclo(Arg-Gly-Asp-D-Phe-Cys)
    		98.08%
    Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors.
  • HY-15102
    MK-0429
    		Antagonist 99.50%
    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
  • HY-100563A
    Cyclo(RGDyK)
    		Inhibitor 99.83%
    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  • HY-P11474
    FZ1 peptide
    		Agonist 99.92%
    FZ1 peptide is an integrin αvβ3 agonist. FZ1 peptide binds to integrin αvβ3, effectively activates FAK, FAK-dependent AKT and ERK1/2 signaling pathways. FZ1 peptide enhances VEGFC-induced endothelial angiogenesis, accelerates diabetic skin wound healing.
  • HY-P11339A
    c-RGD-SH TFA
    		Ligand 98.84%
    c-RGD-SH TFA is an Integrin αvβ3 ligand. c-RGD-SH TFA conjugated with core-crosslinked polymeric micelles (CCPM) can be used for synthesis a dual modality nanoparticle probe, and this probe labeled with both Cy7 and 111In can be used for SPECT and NIRF imaging of tumor.
  • HY-P11424
    Cyclo(GRGDSPA)
    		Inhibitor
    Cyclo(GRGDSPA) is a cyclic RGD peptide targeting αvβ3 integrin. Cyclo(GRGDSPA) reduces the formation of colonies in mice injected with B16-FE7 melanoma cells. Cyclo(GRGDSPA) can be used for melanoma research.
  • HY-19307
    SB-273005
    		Antagonist 99.94%
    SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .
  • HY-P0023A
    Cyclo(-RGDfK) TFA
    		Inhibitor 99.61%
    Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-19767
    GSK 3008348
    		Antagonist 98.04%
    GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.
  • HY-19767A
    GSK 3008348 hydrochloride
    		Antagonist 99.86%
    GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.
  • HY-100563
    Cyclo(RGDyK) trifluoroacetate
    		Inhibitor 99.67%
    Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  • HY-P1187
    HSDVHK-NH2
    		Antagonist 99.54%
    HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).
  • HY-172494
    DSPE-PEG2000-iRGD
    DSPE-PEG2000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG2000-iRGD can be used for agent delivery.
  • HY-172464
    DSPE-PEG2000-cRGD
    DSPE-PEG2000-cRGD is a PEG compound which composed of DSPE and an αvβ3 targeting peptide (cRGD). cRGD peptide can specifically bind to αvβ3 on the surface of many cancer cells and neovascular cells. DSPE-PEG2000-cRGD can be used for drug delivery.
  • HY-P1189A
    Echistatin TFA
    		Antagonist 99.32%
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-P1189
    Echistatin
    		Antagonist
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-P2300A
    Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA
    		Inhibitor 98.69%
    Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA, a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used in the research of tumors.
  • HY-P5021
    Cyclo(Arg-Gly-Asp-(D-Phe)-Glu)
    		99.94%
    Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) c(RGDfE) is a cyclic RGD peptide targeting integrin αvβ3. Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) is commonly used for modifying drug loaded nanoparticles. Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) is often used in cancer research, such as pancreatic cancer.
Cat. No. Product Name / Synonyms Species Source