| 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.
|
-
J Neuroinflammation, 2025, 22(1):168
-
Int J Mol Sci, 2025, 26(6)2465
-
Microbiol Spectr, 2025, 13(2):e0222124
|
|
| 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.
|
-
Nat Commun, 2025, 16(1):2254
-
NPJ Regen Med, 2024, 9(1):4
-
World J Gastroenterol, 2024, 30(7):728-741
|
|
| 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.
|
-
EMBO J, 2025, 10.1038/s44318-025-00565-3
-
bioRxiv, 2025, 2025.04.25.650475
-
Cancer Lett, 2024, 582:216597
|
|
| 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.
|
-
Adv Sci (Weinh), 2025, 12(18):e2417447
-
J Sport Health Sci, 2024, S2095-2546(24)00124-8
-
iScience, 2024, 27(3):109119
|
|
| 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, 2025, 16(1):6531
-
Nat Commun, 2025, 16(1):9183
-
Regen Biomater, 2025, 12:rbaf099
|
|
| S7844 |
Cyclo(RGDyK) TFA
|
Cyclo(RGDyK) TFA is a salt formed by the combination of Cyclo(RGDyK) and trifluoroacetate (TFA). It is an effective and selective Integrin αvβ3 inhibitor with a low IC50 value (e.g., 20 nM). This compound is of great significance in the treatment of cardiovascular diseases, osteoporosis, inflammation and tumors.
|
-
J Clin Invest, 2024, e175147
-
JBMR Plus, 2024, 8(7):ziae066
-
Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7
|
|
| S7834 |
Cyclo(-RGDfK) TFA
|
Cyclo(-RGDfK) TFA is the salt product of Cyclo(-RGDfK) and trifluoroacetic acid (TFA). The addition of TFA enhances stability and biocompatibility. This compound effectively targets tumor microvessels and cancer cells by specifically binding to the cell surface Integrin αvβ3.
|
-
Pharmaceuticals (Basel), 2025, 18(4)549
-
In Vitro Cell Dev Biol Anim, 2025, 10.1007/s11626-025-01101-7
-
Sci Adv, 2024, 10(43):eadp4726
|
|
| 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
-
World J Gastroenterol, 2023, 29(20):3103-3118
|
|
| 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. This compound induces autophagy and apoptosis, both of which are integral to its antiproliferative activity. It 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.
|
-
Nat Commun, 2025, 16(1):5461
-
Signal Transduct Target Ther, 2024, 9(1):109
-
Signal Transduct Target Ther, 2024, 9(1):109
|
|
| E1558 |
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.
|
|
|
| E4615 |
GLPG0187
|
GLPG0187 is a broad-spectrum antagonist of integrin receptor. It inhibits αvβ1-integrin with an IC50 value of 1.3 nM. This compound also inhibits migrasome biogenesis without cytotoxicity. It exhibits potent antitumor activity.
|
-
Sci Rep, 2025, 15(1):9147
|
|
| S4513 |
RGD peptide (GRGDNP)
|
RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. This compound induces apoptosis presumably through direct activation of caspase-3.
|
-
Tradit Med Res, 2023, 8(9):50
|
|
| E0790 |
ILK-IN-3
|
ILK-IN-3 is an integrin linked kinase (ILK) inhibitor with antitumor activity.
|
|
|
| E7334 |
Cyclo(RGDyK)
|
Cyclo(RGDyK) is a potent and selective inhibitor of αVβ3 integrin . It significantly reduces lung inflammation and fibrosis induced by influenza A virus, and improves lung morphology, lowers pulmonary fibrosis scores, and suppresses the expression of αVβ3, TGF-β1, NF-κB p65, p38 MAPK, and HIF-1α, confirming its protective effects against ALI and pulmonary fibrosis.
|
|
|
| E6559New |
GS-1427
|
GS-1427 (Emvistegrast) is an oral, small-molecule quinolone derivative that functions as a potent and selective antagonist of α4β7 integrin, with the potential treatment of inflammatory bowel disease.
|
|
|
| E7759 |
GRGDSP
|
GRGDSP is a fibronectin-derived peptide and an inhibitor of Integrin. It can be used for surface modification of cardiovascular implants, such as vascular grafts, to promote endothelialization, and also holds potential for hepatocellular carcinoma (HCC) treatment by inhibiting tumor cell adhesion and limiting metastasis.
|
|
|
| E1385 |
Bexotegrast (PLN-74809)
|
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.
|
|
|
| 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. |
- J Neuroinflammation, 2025, 22(1):168
- Int J Mol Sci, 2025, 26(6)2465
- Microbiol Spectr, 2025, 13(2):e0222124
|
|
| 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. |
- Nat Commun, 2025, 16(1):2254
- NPJ Regen Med, 2024, 9(1):4
- World J Gastroenterol, 2024, 30(7):728-741
|
|
| 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. |
- EMBO J, 2025, 10.1038/s44318-025-00565-3
- bioRxiv, 2025, 2025.04.25.650475
- Cancer Lett, 2024, 582:216597
|
|
| 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. |
- Adv Sci (Weinh), 2025, 12(18):e2417447
- J Sport Health Sci, 2024, S2095-2546(24)00124-8
- iScience, 2024, 27(3):109119
|
|
| S7844 |
Cyclo(RGDyK) TFA
|
Cyclo(RGDyK) TFA is a salt formed by the combination of Cyclo(RGDyK) and trifluoroacetate (TFA). It is an effective and selective Integrin αvβ3 inhibitor with a low IC50 value (e.g., 20 nM). This compound is of great significance in the treatment of cardiovascular diseases, osteoporosis, inflammation and tumors. |
- J Clin Invest, 2024, e175147
- JBMR Plus, 2024, 8(7):ziae066
- Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7
|
|
| S7834 |
Cyclo(-RGDfK) TFA
|
Cyclo(-RGDfK) TFA is the salt product of Cyclo(-RGDfK) and trifluoroacetic acid (TFA). The addition of TFA enhances stability and biocompatibility. This compound effectively targets tumor microvessels and cancer cells by specifically binding to the cell surface Integrin αvβ3. |
- Pharmaceuticals (Basel), 2025, 18(4)549
- In Vitro Cell Dev Biol Anim, 2025, 10.1007/s11626-025-01101-7
- Sci Adv, 2024, 10(43):eadp4726
|
|
| 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. This compound induces autophagy and apoptosis, both of which are integral to its antiproliferative activity. It 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. This compound induces apoptosis presumably through direct activation of caspase-3. |
- Tradit Med Res, 2023, 8(9):50
|
|
| E0790 |
ILK-IN-3
|
ILK-IN-3 is an integrin linked kinase (ILK) inhibitor with antitumor activity. |
|
|
| E7334 |
Cyclo(RGDyK)
|
Cyclo(RGDyK) is a potent and selective inhibitor of αVβ3 integrin . It significantly reduces lung inflammation and fibrosis induced by influenza A virus, and improves lung morphology, lowers pulmonary fibrosis scores, and suppresses the expression of αVβ3, TGF-β1, NF-κB p65, p38 MAPK, and HIF-1α, confirming its protective effects against ALI and pulmonary fibrosis. |
|
|
| E7759 |
GRGDSP
|
GRGDSP is a fibronectin-derived peptide and an inhibitor of Integrin. It can be used for surface modification of cardiovascular implants, such as vascular grafts, to promote endothelialization, and also holds potential for hepatocellular carcinoma (HCC) treatment by inhibiting tumor cell adhesion and limiting metastasis. |
|
|
| E1385 |
Bexotegrast (PLN-74809)
|
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. |
|
|
| 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, 2025, 16(1):6531
- Nat Commun, 2025, 16(1):9183
- Regen Biomater, 2025, 12:rbaf099
|
|
| 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
- World J Gastroenterol, 2023, 29(20):3103-3118
|
|
| 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
|
|
| E1558 |
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. |
|
|
| E4615 |
GLPG0187
|
GLPG0187 is a broad-spectrum antagonist of integrin receptor. It inhibits αvβ1-integrin with an IC50 value of 1.3 nM. This compound also inhibits migrasome biogenesis without cytotoxicity. It exhibits potent antitumor activity. |
- Sci Rep, 2025, 15(1):9147
|
|
| E6559New |
GS-1427
|
GS-1427 (Emvistegrast) is an oral, small-molecule quinolone derivative that functions as a potent and selective antagonist of α4β7 integrin, with the potential treatment of inflammatory bowel disease. |
|
|