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.

Products
Background
Literature (2)
Gene Data

Integrin Antagonists

Cat. No. Product Name / Activity
6908 TR 14035
Potent integrin α4β7 and α4β1 (VLA-4) antagonist; orally bioavailable

Integrin Modulators

Cat. No. Product Name / Activity
4776 BIRT 377
Potent negative allosteric modulator of LFA-1

Integrin Inhibitors

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

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

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.


    Angiogenesis in Cancer Poster

    Angiogenesis in Cancer Poster

    This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

    Enabling Research By Provision of Chemical Tools Poster

    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.
    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