S7077 |
Cilengitide trifluoroacetate
|
Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2. |
-
Adv Sci (Weinh), 2023, e2307206.
-
Heliyon, 2023, 9(9):e20185
-
Heliyon, 2023, 9(9):e20185
|
|
S6387 |
Cilengitide
|
Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5 with IC50 of 4 and 79 nM, respectively. |
-
NPJ Regen Med, 2024, 9(1):4
-
World J Gastroenterol, 2024, 30(7):728-741
-
Cancer Cell, 2023, 41(8):1480-1497.e9
|
|
S7540 |
SB273005
|
SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
|
-
Cancer Lett, 2024, 582:216597
-
Nat Commun, 2023, 14(1):3251
-
Neuron, 2023, S0896-6273(23)00623-2
|
|
S8008 |
RGD (Arg-Gly-Asp) Peptides
|
RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins. |
-
J Sport Health Sci, 2024, S2095-2546(24)00124-8
-
iScience, 2024, 27(3):109119
-
Cell Stem Cell, 2023, 30(6):867-884.e11
|
|
S8454 |
ATN-161
|
ATN-161 is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
|
-
Nat Commun, 2024, 15(1):5986
-
Int Immunopharmacol, 2024, 141:112947
-
Bioact Mater, 2023, 22:75-90
|
|
S7844 |
Cyclo(RGDyK)
|
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.
|
-
J Clin Invest, 2024, e175147
-
Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7
-
iScience, 2023, 26(6):106839
|
|
S7834 |
Cyclo(-RGDfK) TFA
|
Cyclo(-RGDfK) TFA is a potent and selective αvβ3 integrin inhibitor.
|
-
Sci Adv, 2024, 10(43):eadp4726
-
bioRxiv, 2024, 2024.09.17.613509
-
Oxidative Medicine and Cellular Longevity, 2021, 10.1155/2021/9739977
|
|
S8306 |
Leukadherin-1
|
Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)). |
-
International Immunopharmacology, 2023, Volume 118
-
Int Immunopharmacol, 2023, 118:110024
-
Front Immunol, 2022, 13:919444
|
|
S2885 |
A-205804
|
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively. |
-
Cell Biol Toxicol, 2024, 40(1):90
-
Stem Cell Res Ther, 2022, 13(1):218
-
Am J Rhinol Allergy, 2022, 19458924221086061
|
|
S3714 |
Lifitegrast
|
Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED. |
-
Med Oncol, 2024, 41(8):188
-
World J Gastroenterol, 2023, 29(20):3103-3118
-
Med Chem Res, 2022, 31(4):555-579
|
|
S3085 |
Tirofiban
|
Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM. |
-
Food Funct, 2020, 11(1):139-152
|
|
S8594 |
Tirofiban Hydrochloride
|
Tirofiban Hydrochloride (MK-383) is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Transl Oncol, 2024, 39:101813
-
Front Cell Infect Microbiol, 2021, 11:783085
|
|
S6840 |
OSU-T315
|
OSU-T315 (ILK-IN-2) is a potent Integrin-Linked Kinase (ILK) inhibitor with IC50 of 0.6 μM. OSU-T315 induces autophagy and apoptosis, both of which are integral to its antiproliferative activity. OSU-T315 exhibits anti-tumor activity. |
-
Exp Eye Res, 2023, 234:109609
|
|
E0462 |
Pyrintegrin
|
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival, also enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. |
-
Signal Transduct Target Ther, 2024, 9(1):109
-
Signal Transduct Target Ther, 2024, 9(1):109
|
|
A2420 |
Anti-Integrin b1 / ITGB1 / CD29
|
Anti-Integrin b1 / ITGB1 / CD29 is a humanized monoclonal antibody directed against the human integrin receptor beta-1 subunit (CD29), with potential antineoplastic activity. MW: 145.5 kD. |
|
|
A2873 |
Anti-ICAM3 / CD50
|
Anti-ICAM3 / CD50 is an IgG1 monoclonal antibody against intercellular adhesion molecules-3 (ICAM-3, also known as CD50)) with the potential to have anti-proliferative activities. MW: 145.22 KD. |
|
|
E1558New |
GSK-3008348 HCl
|
GSK-3008348 HCl is a small molecule antagonist of integrin αvβ6 with an affinity (pIC50) value of 8.1 for αvβ6 in cell Adhesion assays. |
|
|
S0314 |
TR-14035
|
TR-14035 (SB 683698, MDK-1191) is a a dual alpha4beta (α4β) integrin antagonist with IC50 of 7 nM and 87 nM for alpha4beta7 (α4β7) and alpha4beta1 (α4β1), respectively. |
|
|
E4615New |
GLPG0187
|
GLPG0187 is a broad-spectrum antagonist of integrin receptor. It inhibits αvβ1-integrin with an IC50 value of 1.3 nM. GLPG0187 also inhibits migrasome biogenesis without cytotoxicity. GLPG0187 exhibits potent antitumor activity. |
|
|
A2464 |
Bersanlimab (Anti-ICAM1 / CD54)
|
Bersanlimab (Anti-ICAM1 / CD54) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects. MW: 145.5 KD. |
|
|
S4513 |
RGD peptide (GRGDNP)
|
RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3. |
|
|
E0790 |
ILK-IN-3
|
ILK-IN-3 is an integrin linked kinase (ILK) inhibitor with antitumor activity. |
|
|
A2704 |
Anti-Integrin aVb6 (ITGAV & ITGB6) (STX-100)
|
Anti-Integrin aVb6 (ITGAV & ITGB6) (STX-100) is a humanized monoclonal antibody directed against the alpha v beta 6 (αvβ6) integrin. It has a potential to be used in research on Idiopathic Pulmonary Fibrosis (IPF). MW : 144.88 kD. |
|
|
A2712 |
Erlizumab (Anti-Integrin b2 / ITGB2 / CD18)
|
Erlizumab (anti-Integrin b2 / ITGB2 / CD18) is a humanized monoclonal antibody targeted against Integrin beta-2 and used as a therapy for hemorrhagic shock. MW: 146.66 kD. |
|
|
A2988 |
Vatelizumab (Anti-Integrin a2b1 (ITGA2 & ITGB1))
|
Vatelizumab (Anti-Integrin a2b1 (ITGA2 & ITGB1)) is a monoclonal antibody targeting the α2 subunit (CD49b) of very late antigen-2 (VLA-2). It can be used for the research of multiple sclerosis. MW: 144.56 KD. |
|
|
A2990 |
Intetumumab (Anti-Integrin aV / ITGAV / CD51)
|
Intetumumab (Anti-Integrin aV / ITGAV / CD51) is a potent monoclonal antibody targeting αV-integrins. It can be used in research of uterine serous papillary carcinoma (USPC) treatment. MW :145.58 KD. |
|
|
A2991 |
Etaracizumab (Anti-Integrin aVb3 (ITGAV & ITGB3))
|
Etaracizumab (Anti-Integrin aVb3 (ITGAV & ITGB3)) is an IgG1 monoclonal antibody targeting αvβ3 integrin. It inhibits angiogenesis and melanoma tumor growth and can be used to research anticancer. MW :144.18 KD. |
|
|
A2744 |
Abituzumab (Anti-Integrin aV / ITGAV / CD51)
|
Abituzumab (Anti-Integrin aV / ITGAV / CD51) is a humanized monoclonal antibody directed against the human alpha v integrin subunit with potential antiangiogenic and antineoplastic activities.MW: 144.78 kD. |
|
|
A2745 |
Anti-Integrin a11 / ITAG11
|
Anti-Integrin a11 / ITAG11 is a monoclonal antibody against Integrin alpha 11 (ITGA11), a transmembrane glycoprotein expressed in adult cardiac and uterine smooth muscle and developing myocytes. MW: 145.7 KD. |
|
|
A2761 |
Abrilumab (Anti-Integrin a4b7 ITGA4 & ITGB7)
|
Abrilumab (Anti-Integrin a4b7 ITGA4 & ITGB7) is a fully human monoclonal immunoglobulin G2 antibody that targets the alpha4beta7 integrin and prevents interaction with MADCAM-1. It has the potential to be used in research on inflammatory bowel disease (IBD). MW: 143.8 kD. |
|
|
E1385New |
Bexotegrast
|
Bexotegrast(PLN-74809) is potent dual selective inhibitor of αvβ6 and αvβ1 integrins with Kd of 5.7 nM and 3.4 nM, respectively. It has antifibrogenic effects, blocks multiple TGF-β activation pathways in the fibrotic lung, and is useful for researching fibrosis, including idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP). |
|
|
S3408 |
A286982
|
A-286982 is a potent, nonpeptide inhibitor of LFA-1/ICAM-1 interaction with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assay, respectively. |
|
|
A2045 |
Vedolizumab (anti-α4β7-integrin)
|
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease. |
|
|
S7077 |
Cilengitide trifluoroacetate
|
Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2. |
- Adv Sci (Weinh), 2023, e2307206.
- Heliyon, 2023, 9(9):e20185
- Heliyon, 2023, 9(9):e20185
|
|
S6387 |
Cilengitide
|
Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5 with IC50 of 4 and 79 nM, respectively. |
- NPJ Regen Med, 2024, 9(1):4
- World J Gastroenterol, 2024, 30(7):728-741
- Cancer Cell, 2023, 41(8):1480-1497.e9
|
|
S7540 |
SB273005
|
SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
|
- Cancer Lett, 2024, 582:216597
- Nat Commun, 2023, 14(1):3251
- Neuron, 2023, S0896-6273(23)00623-2
|
|
S8008 |
RGD (Arg-Gly-Asp) Peptides
|
RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins. |
- J Sport Health Sci, 2024, S2095-2546(24)00124-8
- iScience, 2024, 27(3):109119
- Cell Stem Cell, 2023, 30(6):867-884.e11
|
|
S7844 |
Cyclo(RGDyK)
|
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.
|
- J Clin Invest, 2024, e175147
- Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7
- iScience, 2023, 26(6):106839
|
|
S7834 |
Cyclo(-RGDfK) TFA
|
Cyclo(-RGDfK) TFA is a potent and selective αvβ3 integrin inhibitor.
|
- Sci Adv, 2024, 10(43):eadp4726
- bioRxiv, 2024, 2024.09.17.613509
- Oxidative Medicine and Cellular Longevity, 2021, 10.1155/2021/9739977
|
|
S2885 |
A-205804
|
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively. |
- Cell Biol Toxicol, 2024, 40(1):90
- Stem Cell Res Ther, 2022, 13(1):218
- Am J Rhinol Allergy, 2022, 19458924221086061
|
|
S6840 |
OSU-T315
|
OSU-T315 (ILK-IN-2) is a potent Integrin-Linked Kinase (ILK) inhibitor with IC50 of 0.6 μM. OSU-T315 induces autophagy and apoptosis, both of which are integral to its antiproliferative activity. OSU-T315 exhibits anti-tumor activity. |
- Exp Eye Res, 2023, 234:109609
|
|
S4513 |
RGD peptide (GRGDNP)
|
RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3. |
|
|
E0790 |
ILK-IN-3
|
ILK-IN-3 is an integrin linked kinase (ILK) inhibitor with antitumor activity. |
|
|
E1385New |
Bexotegrast
|
Bexotegrast(PLN-74809) is potent dual selective inhibitor of αvβ6 and αvβ1 integrins with Kd of 5.7 nM and 3.4 nM, respectively. It has antifibrogenic effects, blocks multiple TGF-β activation pathways in the fibrotic lung, and is useful for researching fibrosis, including idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP). |
|
|
S3408 |
A286982
|
A-286982 is a potent, nonpeptide inhibitor of LFA-1/ICAM-1 interaction with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assay, respectively. |
|
|
A2420 |
Anti-Integrin b1 / ITGB1 / CD29
|
Anti-Integrin b1 / ITGB1 / CD29 is a humanized monoclonal antibody directed against the human integrin receptor beta-1 subunit (CD29), with potential antineoplastic activity. MW: 145.5 kD. |
|
|
A2873 |
Anti-ICAM3 / CD50
|
Anti-ICAM3 / CD50 is an IgG1 monoclonal antibody against intercellular adhesion molecules-3 (ICAM-3, also known as CD50)) with the potential to have anti-proliferative activities. MW: 145.22 KD. |
|
|
A2464 |
Bersanlimab (Anti-ICAM1 / CD54)
|
Bersanlimab (Anti-ICAM1 / CD54) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anticancer effects. MW: 145.5 KD. |
|
|
A2704 |
Anti-Integrin aVb6 (ITGAV & ITGB6) (STX-100)
|
Anti-Integrin aVb6 (ITGAV & ITGB6) (STX-100) is a humanized monoclonal antibody directed against the alpha v beta 6 (αvβ6) integrin. It has a potential to be used in research on Idiopathic Pulmonary Fibrosis (IPF). MW : 144.88 kD. |
|
|
A2712 |
Erlizumab (Anti-Integrin b2 / ITGB2 / CD18)
|
Erlizumab (anti-Integrin b2 / ITGB2 / CD18) is a humanized monoclonal antibody targeted against Integrin beta-2 and used as a therapy for hemorrhagic shock. MW: 146.66 kD. |
|
|
A2988 |
Vatelizumab (Anti-Integrin a2b1 (ITGA2 & ITGB1))
|
Vatelizumab (Anti-Integrin a2b1 (ITGA2 & ITGB1)) is a monoclonal antibody targeting the α2 subunit (CD49b) of very late antigen-2 (VLA-2). It can be used for the research of multiple sclerosis. MW: 144.56 KD. |
|
|
A2990 |
Intetumumab (Anti-Integrin aV / ITGAV / CD51)
|
Intetumumab (Anti-Integrin aV / ITGAV / CD51) is a potent monoclonal antibody targeting αV-integrins. It can be used in research of uterine serous papillary carcinoma (USPC) treatment. MW :145.58 KD. |
|
|
A2991 |
Etaracizumab (Anti-Integrin aVb3 (ITGAV & ITGB3))
|
Etaracizumab (Anti-Integrin aVb3 (ITGAV & ITGB3)) is an IgG1 monoclonal antibody targeting αvβ3 integrin. It inhibits angiogenesis and melanoma tumor growth and can be used to research anticancer. MW :144.18 KD. |
|
|
A2744 |
Abituzumab (Anti-Integrin aV / ITGAV / CD51)
|
Abituzumab (Anti-Integrin aV / ITGAV / CD51) is a humanized monoclonal antibody directed against the human alpha v integrin subunit with potential antiangiogenic and antineoplastic activities.MW: 144.78 kD. |
|
|
A2745 |
Anti-Integrin a11 / ITAG11
|
Anti-Integrin a11 / ITAG11 is a monoclonal antibody against Integrin alpha 11 (ITGA11), a transmembrane glycoprotein expressed in adult cardiac and uterine smooth muscle and developing myocytes. MW: 145.7 KD. |
|
|
A2761 |
Abrilumab (Anti-Integrin a4b7 ITGA4 & ITGB7)
|
Abrilumab (Anti-Integrin a4b7 ITGA4 & ITGB7) is a fully human monoclonal immunoglobulin G2 antibody that targets the alpha4beta7 integrin and prevents interaction with MADCAM-1. It has the potential to be used in research on inflammatory bowel disease (IBD). MW: 143.8 kD. |
|
|
A2045 |
Vedolizumab (anti-α4β7-integrin)
|
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease. |
|
|
S8454 |
ATN-161
|
ATN-161 is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
|
- Nat Commun, 2024, 15(1):5986
- Int Immunopharmacol, 2024, 141:112947
- Bioact Mater, 2023, 22:75-90
|
|
S3714 |
Lifitegrast
|
Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED. |
- Med Oncol, 2024, 41(8):188
- World J Gastroenterol, 2023, 29(20):3103-3118
- Med Chem Res, 2022, 31(4):555-579
|
|
S3085 |
Tirofiban
|
Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM. |
- Food Funct, 2020, 11(1):139-152
|
|
S8594 |
Tirofiban Hydrochloride
|
Tirofiban Hydrochloride (MK-383) is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. |
- J Immunother Cancer, 2024, 12(11)e009805
- Transl Oncol, 2024, 39:101813
- Front Cell Infect Microbiol, 2021, 11:783085
|
|
E1558New |
GSK-3008348 HCl
|
GSK-3008348 HCl is a small molecule antagonist of integrin αvβ6 with an affinity (pIC50) value of 8.1 for αvβ6 in cell Adhesion assays. |
|
|
S0314 |
TR-14035
|
TR-14035 (SB 683698, MDK-1191) is a a dual alpha4beta (α4β) integrin antagonist with IC50 of 7 nM and 87 nM for alpha4beta7 (α4β7) and alpha4beta1 (α4β1), respectively. |
|
|
E4615New |
GLPG0187
|
GLPG0187 is a broad-spectrum antagonist of integrin receptor. It inhibits αvβ1-integrin with an IC50 value of 1.3 nM. GLPG0187 also inhibits migrasome biogenesis without cytotoxicity. GLPG0187 exhibits potent antitumor activity. |
|
|