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Integrin Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
Verified customer review of Cilengitide trifluoroacetate
S6387 Cilengitide (EMD 121974) 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
Verified customer review of SB273005
S8008 RGD peptide (Arg-Gly-Asp) 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
Verified customer review of RGD peptide (Arg-Gly-Asp)
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
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
Verified customer review of Cyclo(RGDyK) TFA
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
Verified customer review of A-205804
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
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
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.