Integrins
Integrins are ubiquitously expressed adhesion molecules. They are cell-surface receptors that exist as heterodimers of α and β subunits. Under physiological conditions, integrins are highly glycosylated and contain a Ca2+ or Mg2+ ion, which is essential for ligand binding.
Integrin Antagonists |
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Cat. No. | Product Name / Activity |
6908 | TR 14035 |
Potent integrin α4β7 and α4β1 (VLA-4) antagonist; orally bioavailable | |
Integrin Modulators |
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Cat. No. | Product Name / Activity |
4776 | BIRT 377 |
Potent negative allosteric modulator of LFA-1 | |
Integrin Inhibitors |
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Cat. No. | Product Name / Activity |
2524 | A 205804 |
Selective inhibitor of E-selectin and ICAM-1 expression | |
4228 | A 286982 |
Potent inhibitor of the LFA-1/ICAM-1 interaction | |
6058 | ATN 161 |
α5β1 integrin receptor antagonist | |
3910 | BIO 1211 |
Selective α4β1 (VLA-4) inhibitor | |
5051 | BIO 5192 |
Highly potent and selective inhibitor of integrin α4β1 (VLA-4) | |
4970 | BMS 688521 |
Potent inhibitor of the LFA-1/ICAM interaction | |
6047 | BOP |
Dual α9β1/α4β1 integrin inhibitor; preferentially mobilizes HSCs | |
4724 | BTT 3033 |
Selective inhibitor of integrin α2β1 | |
5870 | Cilengitide |
Potent and selective inhibitor of integrins αvβ3 and αvβ5 | |
6785 | E 7820 |
α2 integrin inhibitor; anti-angiogenic | |
3202 | Echistatin, α1 isoform |
αVβ3 and glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor | |
7508 | EMD 527040 hydrochloride |
ανβ6 integrin inhibitor | |
7059 | GLPG 0187 |
Potent αv integrin inhibitor | |
1263 | GR 144053 trihydrochloride |
Glycoprotein IIb/IIIa (integrin αIIbβ3) receptor antagonist. Antithrombotic | |
5114 | K34c |
Potent and selective α5β1 integrin inhibitor | |
4664 | Obtustatin |
Potent and selective α1β1 inhibitor | |
3498 | RGDS peptide |
Integrin binding sequence; inhibits integrin receptor function | |
4527 | TC-I 15 |
Potent α2β1 inhibitor; displays antithrombotic activity in vivo | |
3900 | TCS 2314 |
α4β1 (VLA-4) antagonist | |
Ligands |
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Cat. No. | Product Name / Activity |
8042 | Alkyne-cRGD |
Integrin ligand for degrader development and targeted delivery, with alkyne click handle for conjugation | |
7020 | LDV |
α4β1 (VLA-4) ligand | |
Other |
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Cat. No. | Product Name / Activity |
6996 | BOP-JF549 |
Yellow fluorescent dual α9β1/α4β1 integrin inhibitor comprising BOP conjugated to Janelia Fluor® 646; fluorogenic; photostable | |
6997 | BOP-JF646 |
Red fluorescent dual α9β1/α4β1 integrin inhibitor comprising BOP conjugated to Janelia Fluor® 646; fluorogenic; photostable | |
4577 | LDV FITC |
Fluorescent ligand for α4β1 (VLA-4) |
Integrins are ubiquitously expressed adhesion molecules. They are cell-surface receptors that exist as heterodimers of α and β subunits. Under physiological conditions, integrins are highly glycosylated and contain a Ca2+ or Mg2+ ion, which is essential for ligand binding.
Integrins 'integrate' the extracellular environment with the cell interior by binding both the extracellular matrix (ECM) and the cytoskeleton. They are critical for cell attachment to the ECM, which is mediated through integrin-fibronectin, -vitronectin, -collagen and -laminin interactions. Intracellularly, integrins form adhesion complexes with proteins including talin, vinculin, paxillin and α-actinin. They also regulate kinases, such as focal adhesion kinase and Src family kinases, to mediate attachment to the actin cytoskeleton. Integrins also have a significant role in cell signaling and can activate protein kinases involved in the regulation of cell growth, division, survival, differentiation, migration and apoptosis.
Glycoprotein II/IIIb (αIIbβ3) is an integrin receptor found on the surface of platelets. It is involved in the cross-linking of platelets with fibrin, and so has a vital role in blood clot formation.
External sources of pharmacological information for Integrins :
Literature for Integrins
Tocris offers the following scientific literature for Integrins to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Enabling Research By Provision of Chemical Tools Poster
The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.Integrin Gene Data
Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
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α1 | Human | ITGA1 | NM_181501 | P56199 |
Mouse | Itga1 | NM_001033228 | Q3V3R4 | |
Rat | Itga1 | NM_030994 | P18614 | |
α2 | Human | ITGA2 | NM_002203 | P17301 |
Mouse | Itga2 | NM_008396 | Q62469 | |
Rat | Itga2 | XM_345156 | Q924S3 | |
α3 | Human | ITGA3 | NM_005501 | P26006 |
Mouse | Itga3 | NM_013565 | Q62470 | |
Rat | Itga3 | NM_001108292 | XP_340885 | |
α4 | Human | IGTA4 | NM_000885 | P13612 |
Mouse | Igta4 | NM_010576 | Q00651 | |
Rat | Igta4 | NM_001107737 | XP_230033 | |
α5 | Human | ITGA5 | NM_002205 | P08648 |
Mouse | Itga5 | NM_010577 | P11688 | |
Rat | Itga5 | NM_001108118 | Q7M074 | |
α6 | Human | ITGA6 | NM_001079818 | Q53RX7 |
Mouse | Itga6 | NM_008397 | Q61739 | |
Rat | Igta6 | XM_215984 | Q924W3 | |
α7 | Human | ITGA7 | NM_002206 | Q13683 |
Mouse | Itga7 | NM_008398 | Q61738 | |
Rat | Itga7 | NM_030842 | Q63258 | |
α8 | Human | ITGA8 | NM_003638 | P53708 |
Mouse | Itga8 | NM_001001309 | A2ARA8 | |
Rat | Itga8 | AF148797 | Q9WUP8 | |
α9 | Human | ITGA9 | NM_002207 | Q13797 |
Mouse | Itga9 | NM_133721 | NP_598482 | |
Rat | Itga9 | XM_001061864 | XP_001061864 | |
α10 | Human | ITGA10 | NM_003637 | O75578 |
Mouse | Itga10 | NM_001081053 | NP_001074522 | |
Rat | Itga10 | NM_001107699 | XP_227469 | |
α11 | Human | ITGA11 | NM_012211 | Q9UKX5 |
Mouse | Itga11 | NM_176922 | P61622 | |
Rat | Itga11 | NM_001108156 | XP_236320 | |
αD | Human | ITGAD | NM_005353 | Q13349 |
Mouse | Itgad | NM_001029872 | Q3V0T4 | |
Rat | Itgad | NM_031691 | Q9QYE7 | |
αE | Human | ITGAE | NM_002208 | P38570 |
Mouse | Itgae | NM_008399 | Q60677 | |
Rat | Itgae | NM_031768 | O88340 | |
αL | Human | ITGAL | NM_002209 | P20701 |
Mouse | Itgal | NM_008400 | P24063 | |
Rat | Itgal | NM_001033998 | Q3T1L6 | |
αM | Human | ITGAM | NM_000632 | P11215 |
Mouse | Itgam | NM_001082960 | P05555 | |
Rat | Igtam | NM_012711 | Q9JI30 | |
αV | Human | ITGAV | NM_002210 | P06756 |
Mouse | Itgav | NM_008402 | P43406 | |
Rat | Itgav | NM_001106549 | XP_230950 | |
αX | Human | ITGAX | NM_000887 | P20702 |
Mouse | Itgax | NM_021334 | Q9QXH4 | |
Rat | Itgax | XM_574569 | XP_574569 | |
β1 | Human | ITGB1 | NM_002211 | Q14622 |
Mouse | Itgb1 | NM_010578 | P09055 | |
Rat | Itgb1 | NM_017022 | P49134 | |
β2 | Human | ITGB2 | NM_000211 | P05107 |
Mouse | Itgb2 | NM_008404 | P11835 | |
Rat | Itgb2 | NM_001037780 | Q4KLK5 | |
β3 | Human | ITGB3 | NM_000212 | P05106 |
Mouse | Itgb3 | NM_016780 | O54890 | |
Rat | Itgb3 | NM_153720 | Q8R2H2 | |
β4 | Human | ITGB4 | NM_001005731 | P16144 |
Mouse | Itgb4 | NM_001005608 | NP_001005608 | |
Rat | Itgb4 | NM_013180 | Q64632 | |
β5 | Human | ITGB5 | NM_002213 | P18084 |
Mouse | Itgb5 | NM_010580 | O70309 | |
Rat | Itgb5 | NM_147139.2 | Q8VIM7 | |
β6 | Human | ITGB6 | NM_000888 | P18564 |
Mouse | Itgb6 | NM_021359 | Q9Z0T9 | |
Rat | Itgb6 | NM_001004263 | Q6AYF4 | |
β7 | Human | ITGB7 | NM_000889 | P26010 |
Mouse | Itgb7 | NM_013566 | P26011 | |
Rat | Itgb7 | XM_343336 | Q4G029 | |
β8 | Human | ITGB8 | NM_002214 | P26012 |
Mouse | Itgb8 | NM_177290 | NP_796264 | |
Rat | Itgb8 | NM_001108726 | XP_343127 |