Integrin
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Integrin Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7077 |
Cilengitide trifluoroacetateCilengitide 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. |
Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Cilengitide. Cilengitide is based on the cyclic peptide cyclo(-RGDfV-), which is selective for αv integrins. Interestingly, it acts differently on HTB183 and A549 cell lines. Cilengitide was more efficient on A549, lung adenocarcinoma, while in HTB183 it showed moderate inhibitory activity. This may be due to the mestastatic nature of HTB183 cells which have already lost the cell adhesion properties.
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| S8008 |
RGD (Arg-Gly-Asp) PeptidesRGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins. |
Observation of actin cytoskeleton and nucleus of MC3T3-E1 cells cultured in the presence of different inhibitors (Control, EDTA, RGD, MAB1998, IgG and Heparin) after 24 hours of incubation.
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| S2885 |
A-205804A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively. |
The effect of rhICAM-1 or inhibitor A-205804 on hepsin or CtsD transfected MCF-7 cells was detected. The level of E-cadherin, claudin-1, N-cadherin, vimentin and Snail1 was analyzed by western blot.
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| S7540 |
SB273005SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively. |
Western blot analysis of levels of p-FAK (Tyr397) and total FAK in SK-N-SH cells treated with SB273005 (3 μM) for 6 h and 24 h. One experiment is shown for each cell line. Control cells (treated with diluent, marked as C, were also included). α-tubulin was used as the reference protein.
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| S6840New |
OSU-T315OSU-T315 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. |
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| S7834 |
Cyclo (-RGDfK)Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor. |
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| S7844 |
Cyclo(RGDyK)Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM. |
(E, F) Inhibition of integrin pathway by integrin inhibitor Cyclo(RGDyK) (30 µM) eliminated the enhancement of ZC3H14 depletion on integrin pathway in HepG2 (E) and MHCC-97L (F) cells. NS, non-specific reactive band.
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| S3085 |
TirofibanTirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM. |
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| S0314New |
TR-14035TR-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. |
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| S8594 |
Tirofiban HydrochlorideTirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. |
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| S8454 |
ATN-161 (Ac-PHSCN-NH2)ATN-161 (Ac-PHSCN-NH2) 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. |
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| S3714 |
LifitegrastLifitegrast is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED. |
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| S8306 |
Leukadherin-1Leukadherin-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)). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7077 |
Cilengitide trifluoroacetateCilengitide 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. |
Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Cilengitide. Cilengitide is based on the cyclic peptide cyclo(-RGDfV-), which is selective for αv integrins. Interestingly, it acts differently on HTB183 and A549 cell lines. Cilengitide was more efficient on A549, lung adenocarcinoma, while in HTB183 it showed moderate inhibitory activity. This may be due to the mestastatic nature of HTB183 cells which have already lost the cell adhesion properties.
|
|
| S8008 |
RGD (Arg-Gly-Asp) PeptidesRGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins. |
Observation of actin cytoskeleton and nucleus of MC3T3-E1 cells cultured in the presence of different inhibitors (Control, EDTA, RGD, MAB1998, IgG and Heparin) after 24 hours of incubation.
|
|
| S2885 |
A-205804A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively. |
The effect of rhICAM-1 or inhibitor A-205804 on hepsin or CtsD transfected MCF-7 cells was detected. The level of E-cadherin, claudin-1, N-cadherin, vimentin and Snail1 was analyzed by western blot.
|
|
| S7540 |
SB273005SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively. |
Western blot analysis of levels of p-FAK (Tyr397) and total FAK in SK-N-SH cells treated with SB273005 (3 μM) for 6 h and 24 h. One experiment is shown for each cell line. Control cells (treated with diluent, marked as C, were also included). α-tubulin was used as the reference protein.
|
|
| S6840New |
OSU-T315OSU-T315 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. |
||
| S7834 |
Cyclo (-RGDfK)Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor. |
||
| S7844 |
Cyclo(RGDyK)Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM. |
(E, F) Inhibition of integrin pathway by integrin inhibitor Cyclo(RGDyK) (30 µM) eliminated the enhancement of ZC3H14 depletion on integrin pathway in HepG2 (E) and MHCC-97L (F) cells. NS, non-specific reactive band.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3085 |
TirofibanTirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM. |
||
| S0314New |
TR-14035TR-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. |
||
| S8594 |
Tirofiban HydrochlorideTirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban. |
||
| S8454 |
ATN-161 (Ac-PHSCN-NH2)ATN-161 (Ac-PHSCN-NH2) 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. |
||
| S3714 |
LifitegrastLifitegrast is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8306 |
Leukadherin-1Leukadherin-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)). |
