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Integrin Inhibitor

" in MedChemExpress (MCE) Product Catalog:

168

Inhibitors & Agonists

3

Biochemical Assay Reagents

47

Peptides

13

Inhibitory Antibodies

5

Natural
Products

4

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0023
    Cyclo(-RGDfK)
    Maximum Cited Publications
    27 Publications Verification

    Integrin Cancer
    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 .
    Cyclo(-RGDfK)
  • HY-100506
    GLPG0187
    15+ Cited Publications

    Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM . GLPG0187 inhibits migrasome biogenesis without cytotoxicity .
    GLPG0187
  • HY-100563A
    Cyclo(RGDyK)
    4 Publications Verification

    Integrin Cancer
    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
    Cyclo(RGDyK)
  • HY-13535
    ATN-161
    5+ Cited Publications

    Integrin Cancer
    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161
  • HY-12290
    Arg-Gly-Asp-Ser
    5+ Cited Publications

    RGDS peptide; Fibronectin tetrapeptide

    Integrin Inflammation/Immunology
    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.
    Arg-Gly-Asp-Ser
  • HY-13535A
    ATN-161 trifluoroacetate salt
    5+ Cited Publications

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
    ATN-161 trifluoroacetate salt
  • HY-18644
    CWHM-12
    5+ Cited Publications

    Integrin Cancer
    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.
    CWHM-12
  • HY-177080

    GS-1427

    Integrin Inflammation/Immunology
    Emvistegrast (GS-1427) is a quinolone derivative. Emvistegrast is also an inhibitor of α4β7 integrin. Emvistegrast can be used to investigate diseases mediated by α4β7 integrin, such as inflammatory bowel disease .
    Emvistegrast
  • HY-P0023A
    Cyclo(-RGDfK) TFA
    Maximum Cited Publications
    27 Publications Verification

    Integrin Cancer
    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 .
    Cyclo(-RGDfK) TFA
  • HY-107589
    BIO5192
    2 Publications Verification

    Integrin Inflammation/Immunology
    BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
    BIO5192
  • HY-16143
    Cilengitide TFA
    Maximum Cited Publications
    70 Publications Verification

    EMD 121974 TFA

    Integrin Autophagy Cancer
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
    Cilengitide TFA
  • HY-164957

    SGN-B6A; PF-08046047

    Antibody-Drug Conjugates (ADCs) Integrin Cancer
    SGN-B6A is an ADC, which targets integrin beta-6 (ITGB6) through human IgG1 monoclonal antibody Sigvotatug (HY-P990764), and exhibits cytotoxicity against multiple integrin beta-6-positive cancer cell through mitotic inhibitor MMAE (HY-15162) .
    Sigvotatug vedotin
  • HY-14857

    HCA2969

    Integrin Inflammation/Immunology
    Carotegrast (HCA2969) is an orally active α4 integrin inhibitor with anti-inflammatory activity. Carotegrast can be used in the research of inflammation-related diseases, such as ulcerative colitis .
    Carotegrast
  • HY-P0290
    GRGDSP
    5 Publications Verification

    Integrin Cancer
    GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
    GRGDSP
  • HY-P99333
    Volociximab
    2 Publications Verification

    M200; Eos 200-4

    Integrin Cardiovascular Disease Cancer
    Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs) .
    Volociximab
  • HY-P990203

    Integrin Inflammation/Immunology
    Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) is a rat-derived anti-LPAM-1/Integrin α4β7 IgG2a, κ type antibody inhibitor. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) specifically reacts with both chains of the α4β7 heterodimer and blocks the adhesion to immobilized mucosal addressin cell adhesion molecule-1 (MAdCAM-1). Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) suppresses the proliferation and cytokine secretion of CD8+ T cells. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) decreases Peyer’s patches and follicular B cells in mice. Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32) can be used for the researches of inflammation, such as ulcerative colitis .
    Anti-Mouse LPAM-1/Integrin α4β7 Antibody (DATK32)
  • HY-100445A
    αvβ1 integrin-IN-1 TFA
    5+ Cited Publications

    Integrin Cardiovascular Disease Cancer
    αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects .
    αvβ1 integrin-IN-1 TFA
  • HY-100563
    Cyclo(RGDyK) trifluoroacetate
    4 Publications Verification

    Integrin Cancer
    Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
    Cyclo(RGDyK) trifluoroacetate
  • HY-P5133
    Synstatin (92-119)
    1 Publications Verification

    SSTN92-119

    Integrin Cancer
    Synstatin (92-119) is an inhibitor of αvβ3/αvβ5 integrins and IGF1R with anti-angiogenic, anti-proliferative, antioxidant and anti-tumor activities. Synstatin (92-119) competitively blocks the capture of αvβ3/αvβ5 integrins and IGF1R by syndecan-1, disrupts the formation of the syndecan-1 : integrin : IGF1R ternary complex, inhibits integrin activation and talin-mediated signaling pathways, and blocks VEGF-induced angiogenesis. Synstatin (92-119) is applicable to research related to cancer and hepatocellular carcinoma .
    Synstatin (92-119)
  • HY-P1408
    Obtustatin
    4 Publications Verification

    Integrin VEGFR Cancer
    Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma .
    Obtustatin
  • HY-19767
    GSK 3008348
    2 Publications Verification

    Integrin TGF-β Receptor Infection Inflammation/Immunology Cancer
    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 .
    GSK 3008348
  • HY-19307

    Integrin Interleukin Related Cardiovascular Disease Inflammation/Immunology Endocrinology Cancer
    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. .
    SB-273005
  • HY-70073
    Zaurategrast
    3 Publications Verification

    CT7758

    Integrin Inflammation/Immunology
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor .
    Zaurategrast
  • HY-100445
    αvβ1 integrin-IN-1
    5+ Cited Publications

    Integrin Cardiovascular Disease Cancer
    αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects .
    αvβ1 integrin-IN-1
  • HY-P0322

    EMD 56574

    Integrin Cardiovascular Disease Metabolic Disease
    GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
    GRGDSPK
  • HY-145363
    αvβ5 integrin-IN-1
    1 Publications Verification

    Integrin Cancer
    αvβ5 integrin-IN-1 (Compound 12) is a selective αvβ5 inhibitor (pIC50 = 8.2). αvβ5 integrin-IN-1 exhibits 800-fold selectivity for αvβ5 versus αvβ3 .
    αvβ5 integrin-IN-1
  • HY-P5098

    Integrin Neurological Disease Cancer
    E (c (RGDfK)) 2 is a αvβ3 integrin ligand and tumor-targeting agent. E (c (RGDfK)) 2 binds to αvβ3 integrin, mediates receptor-mediated endocytosis of conjugated payloads, and inhibits integrin-dependent cell adhesion to fibrinogen. E (c (RGDfK)) 2 inhibits the proliferation of cancer cells and endothelial cells. E (c (RGDfK)) 2 preferentially accumulates in orthotopic mouse breast tumors and human ovarian cancer xenograft tumors. E (c (RGDfK)) 2 can be used in research related to glioblastoma, lung cancer, breast adenocarcinoma and ovarian cancer .
    E(c(RGDfK))2
  • HY-115677

    Ser/Thr Kinase Cancer
    ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model .
    ILK-IN-3
  • HY-P99296

    CNTO 95; Anti-Human CD51 Recombinant Antibody

    Integrin Apoptosis Cancer
    Intetumumab (CNTO 95) is a human monoclonal antibody targeting αv integrin, with a Kd value of 1-24 nM. Through high-affinity binding to αv integrin, Intetumumab inhibits its interaction with extracellular matrix proteins (such as vitronectin and fibronectin), thereby blocking the downstream focal adhesion kinase signaling pathway. This further inhibits the adhesion, migration and invasion of tumor cells as well as the proliferation of vascular endothelial cells, promotes cell apoptosis, and exerts anti-tumor and anti-angiogenic effects. Intetumumab can be used in research related to head and neck cancer, non-small cell lung cancer and uterine serous papillary carcinoma .
    Intetumumab
  • HY-P1654

    Integrin Cancer
    A20FMDV2 is a highly selective αvβ6 integrin inhibitor with human IC50 values of 3 nM and binds with at least 1000-fold selectivity over other RGD-binding integrins. A20FMDV2 binds to the integrin’s RGD-binding site, induces rapid integrin internalization, and delays post-internalization integrin recycling to the cell surface. A20FMDV2 can be used for the research of pancreatic cancer, breast cancer, colorectal cancer, ovarian cancer, oral squamous cell carcinoma .
    A20FMDV2
  • HY-130119

    Integrin Cancer
    Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively .
    Integrin-IN-2
  • HY-150124

    Integrin Apoptosis Cancer
    K34c is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c can be used in glioblastoma research .
    K34c
  • HY-19767A
    GSK 3008348 hydrochloride
    2 Publications Verification

    Integrin TGF-β Receptor Infection Inflammation/Immunology Cancer
    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 .
    GSK 3008348 hydrochloride
  • HY-P4896

    Integrin Cancer
    FITC-Ahx Gly Arg Gly Asp Ser Pro is a GRGDSP (HY-P0290) coupled to FITC. GRGDSP is an integrin inhibitor that can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis .
    FITC-Ahx-Gly-Arg-Gly-Asp-Ser-Pro
  • HY-P10045

    Integrin Cardiovascular Disease
    Integrin signaling inhibitor, mP13 is an inhibitor of integrin signaling. Integrin signaling inhibitor, mP13 inhibits inside-out and outside-in signaling, including fibrinogen binding, platelet adhesion, and clot retraction .
    Integrin signaling inhibitor, mP13
  • HY-W008201

    Drug Intermediate Inflammation/Immunology
    tert-Butyl 3-formylpyrrolidine-1-carboxylate is a drug intermediate that can be used for the synthesis nonpeptidic αvβ6 Integrin inhibitors .
    tert-Butyl 3-formylpyrrolidine-1-carboxylate
  • HY-P0178

    Integrin Inflammation/Immunology
    LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
    LXW7
  • HY-107589A
    BIO5192 hydrate
    2 Publications Verification

    Integrin Inflammation/Immunology
    BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
    BIO5192 hydrate
  • HY-129453

    Integrin Inflammation/Immunology
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
    BOP sodium
  • HY-P0290A
    GRGDSP TFA
    5 Publications Verification

    Integrin Cancer
    GRGDSP (TFA) is an integrin inhibitor.
    GRGDSP TFA
  • HY-172888

    Endogenous Metabolite Sialyltransferase FAK Integrin Cancer
    SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer .
    SPP-037
  • HY-161730

    Integrin Cardiovascular Disease Cancer
    αvβ1 integrin-IN-3 is a selective αvβ1 integrin inhibitor. αvβ1 integrin-IN-3 has an antifibrotic effect .
    αvβ1 integrin-IN-3
  • HY-16031

    NSC710464 free base

    Aryl Hydrocarbon Receptor Integrin Drug Intermediate DNA/RNA Synthesis Cancer
    AFP464 (NSC710464) free base is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 free base downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 free base is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 free base is applicable to research related to breast cancer .
    AFP464 free base
  • HY-P10038A

    Myr-FEEERA-OH TFA

    Integrin Infection
    mP6 (Myr-FEEERA-OH) TFA is a myristoylated peptide. mP6 TFA inhibits the interaction of Gα13 with integrin β3 without disrupting talin-dependent integrin function. mP6 TFA can block the GTP usage of Rac1, Rap1, and Rab7, effectively inhibiting the infection of CHO-A24 cells .
    mP6 TFA
  • HY-P0178A

    Integrin Inflammation/Immunology
    LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
    LXW7 TFA
  • HY-125053A

    Glycoprotein VI Cardiovascular Disease
    Batifiban TFA, a cyclic peptide, is an antagonist of platelet glycoprotein GPⅡb/Ⅲa and inhibits platelet aggregation. Batifiban blocks the binding of circulating vitronectin to integrin ανβ3 .
    Batifiban TFA
  • HY-162558

    Factor Xa Cardiovascular Disease
    NCGC00351170 is an antiplatelet agent that disrupts the calcium and integrin-binding protein 1 (CIB1)-αIIbβ3 interaction. NCGC00351170 inhibits thrombin-induced human platelet aggregation .
    NCGC00351170
  • HY-P1408A
    Obtustatin triacetate
    4 Publications Verification

    Integrin Cancer
    Obtustatin triacetate is a 41-residue non-RGD disintegrin. Obtustatin triacetate can be isolated from the venom of Vipera lebetina obtusa. Obtustatin triacetate is a potent and selective inhibitor of integrin α1β1 adhesion to type IV collagen. Obtustatin triacetate inhibits angiogenesis and may be used in cancer research .
    Obtustatin triacetate
  • HY-102073

    Glutaminase Integrin FAK Src Cancer
    TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research .
    TG53
  • HY-153807

    Integrin Inflammation/Immunology
    αvβ6 integrin inhibitor 2 is a potent ανβ6 integrin inhibitor with an IC50 of 96.5 nM (WO2020081154A1, example 19) .
    αvβ6 integrin inhibitor 2

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