Integrin

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Integrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated as crucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family, including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appear to promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, the functions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling, including the PI3K/Akt- and Ras/MAPK-dependent pathways.

Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulation of these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state. Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process via activation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.

Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one β subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit can form heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, and αv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be a common function of multiple αv integrins.

Integrin Isoform Specific Products:

Integrin Isoform Comparison

Integrin Related Products (236)
Recombinant Proteins (21)
Antibodies (31)
Integrin Isoform Comparison

By Effects:	Ligand (1) Inhibitors (112) Agonists (5) Antagonists (57) Activators (3) Modulators (4) Chemicals (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-16141

Cilengitide	Antagonist	99.80%
Cilengitide (EMD 121974) is a potent integrins antagonist with IC₅₀s of 0.61 nM (α_νβ₃), 8.4 nM (α_νβ₅) and 14.9 nM (α₅β₁), respectively. Cilengitide inhibits the binding of α_νβ₃ and α_νβ₅ 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	≥98.0%
Cyclo(-RGDfK) is a potent and selective inhibitor of the α_vβ₃ 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-P3160

Fibronectin	Modulator
Fibronectin, a glycoprotein present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans.

HY-N0416

Cucurbitacin B	Inhibitor	99.91%
Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.

HY-100506

GLPG0187	Antagonist	99.43%
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

HY-P990764

Sigvotatug	Ligand
Sigvotatug is an anti-ITGB6 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

HY-P1654

A20FMDV2	Inhibitor	98.03%
A20FMDV2 is a selective αvβ6 integrin inhibitor (IC₅₀: 3 nM), with an activity 1,000-fold more selective for αvβ6 than for other RGD-directed integrins (αvβ3, αvβ5, and α5β1). A20FMDV2 can be derived from the foot-and-mouth disease virus. A20FMDV2 can be radiolabeled for the PET imaging of αvβ6 integrin-positive tumors.

HY-164768

LT25	Agonist	98.73%
LT25 (compound 17) is a agonist of α5β1 integrin with EC₅₀ value of 9.9 nM.

HY-137561

Bexotegrast	Inhibitor	98.94%
Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with K_d of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC₅₀ values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung.

HY-14571

E7820	Inhibitor	99.06%
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC₅₀ of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.

HY-13306

Pyrintegrin	Agonist	99.41%
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.

HY-P0278

RGD		98.37%
RGD is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; binds to integrins.

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-12290

Arg-Gly-Asp-Ser	Inhibitor	99.93%
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.

HY-13535A

ATN-161 trifluoroacetate salt	Antagonist	99.04%
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.

HY-18644

CWHM-12	Inhibitor	99.94%
CWHM-12 is a potent inhibitor of αV integrins with IC₅₀s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.

HY-19344

Lifitegrast	Antagonist	99.29%
Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM. Lifitegrast can be used for researching dry eye disease.

HY-100445A

αvβ1 integrin-IN-1 TFA	Inhibitor	98.04%
αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC₅₀ of 0.63 nM. Antifibrotic effects.

HY-P0074

GPRP		99.89%
GPRP (Pefa 6003) is a fibrin polymerization inhibitor that inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa).

HY-100226

A-205804	Inhibitor	98.12%
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC₅₀ of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.

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Integrin

Integrin

Integrin Isoform Specific Products:

Integrin Isoform Specific Products:

Integrin Related Products (236)

Recombinant Proteins (21)

Antibodies (31)

Integrin Isoform Comparison

Integrin Related Products (236):