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TargetIntegrin alpha-4/beta-1 [T112H]
LigandBDBM17924
Substrate/CompetitorEu-Labeled Human VCAM-1/Fc Chimera
Meas. Tech.VLA-4/VCAM-1 binding assay
pH7.5±n/a
Temperature295.15±n/a K
IC50 1.1±n/a nM
Citation Chiba, JTakayama, GTakashi, TYokoyama, MNakayama, ABaldwin, JJMcDonald, EMoriarty, KJSarko, CRSaionz, KWSwanson, RHussain, ZWong, AMachinaga, N Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists. Bioorg Med Chem14:2725-46 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Integrin alpha-4/beta-1 [T112H]
Name:Integrin alpha-4/beta-1 [T112H]
Synonyms:CD49d/CD29 | Integrin alpha4beta1 (VLA-4) | Very Late Antigen-4
Type:Protein Complex
Mol. Mass.:n/a
Description:The assay uses transfected Ramos cells expressing alpha4beta1 integrin.
Components:This complex has 2 components.
Component 1
Name:Integrin alpha-4
Synonyms:CD49 antigen-like family member D | CD49D | CD49d antigen | CD_antigen=CD49d | ITA4_HUMAN | ITGA4 | Integrin alpha-4 | Integrin alpha-4/beta-7 | Integrin alpha-IV | Integrin alpha4 | VLA-4 | VLA-4 subunit alpha | integrin alpha 4 precursor | integrin alpha-4 precursor
Type:Membrane Protein
Mol. Mass.:114897.35
Organism:Homo sapiens (Human)
Description:P13612
Residue:1032
Sequence:
MAWEARREPGPRRAAVRETVMLLLCLGVPTGRPYNVDTESALLYQGPHNTLFGYSVVLHS
HGANRWLLVGAPTANWLANASVINPGAIYRCRIGKNPGQTCEQLQLGSPNGEPCGKTCLE
ERDNQWLGVTLSRQPGENGSIVTCGHRWKNIFYIKNENKLPTGGCYGVPPDLRTELSKRI
APCYQDYVKKFGENFASCQAGISSFYTKDLIVMGAPGSSYWTGSLFVYNITTNKYKAFLD
KQNQVKFGSYLGYSVGAGHFRSQHTTEVVGGAPQHEQIGKAYIFSIDEKELNILHEMKGK
KLGSYFGASVCAVDLNADGFSDLLVGAPMQSTIREEGRVFVYINSGSGAVMNAMETNLVG
SDKYAARFGESIVNLGDIDNDGFEDVAIGAPQEDDLQGAIYIYNGRADGISSTFSQRIEG
LQISKSLSMFGQSISGQIDADNNGYVDVAVGAFRSDSAVLLRTRPVVIVDASLSHPESVN
RTKFDCVENGWPSVCIDLTLCFSYKGKEVPGYIVLFYNMSLDVNRKAESPPRFYFSSNGT
SDVITGSIQVSSREANCRTHQAFMRKDVRDILTPIQIEAAYHLGPHVISKRSTEEFPPLQ
PILQQKKEKDIMKKTINFARFCAHENCSADLQVSAKIGFLKPHENKTYLAVGSMKTLMLN
VSLFNAGDDAYETTLHVKLPVGLYFIKILELEEKQINCEVTDNSGVVQLDCSIGYIYVDH
LSRIDISFLLDVSSLSRAEEDLSITVHATCENEEEMDNLKHSRVTVAIPLKYEVKLTVHG
FVNPTSFVYGSNDENEPETCMVEKMNLTFHVINTGNSMAPNVSVEIMVPNSFSPQTDKLF
NILDVQTTTGECHFENYQRVCALEQQKSAMQTLKGIVRFLSKTDKRLLYCIKADPHCLNF
LCNFGKMESGKEASVHIQLEGRPSILEMDETSALKFEIRATGFPEPNPRVIELNKDENVA
HVLLEGLHHQRPKRYFTIVIISSSLLLGLIVLLLISYVMWKAGFFKRQYKSILQEENRRD
SWSYINSKSNDD
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Component 2
Name:Integrin beta-1 [T112H]
Synonyms:CD29 antigen | FNRB | Fibronectin receptor subunit beta | ITB1_HUMAN | ITGB1 | Integrin VLA-4 subunit beta | Integrin beta1 | MDF2 | MSK12
Type:Membrane Protein
Mol. Mass.:88450.95
Organism:Homo sapiens (Human)
Description:P05556[T112H]
Residue:798
Sequence:
MNLQPIFWIGLISSVCCVFAQTDENRCLKANAKSCGECIQAGPNCGWCTNSTFLQEGMPT
SARCDDLEALKKKGCPPDDIENPRGSKDIKKNKNVTNRSKGTAEKLKPEDIHQIQPQQLV
LRLRSGEPQTFTLKFKRAEDYPIDLYYLMDLSYSMKDDLENVKSLGTDLMNEMRRITSDF
RIGFGSFVEKTVMPYISTTPAKLRNPCTSEQNCTTPFSYKNVLSLTNKGEVFNELVGKQR
ISGNLDSPEGGFDAIMQVAVCGSLIGWRNVTRLLVFSTDAGFHFAGDGKLGGIVLPNDGQ
CHLENNMYTMSHYYDYPSIAHLVQKLSENNIQTIFAVTEEFQPVYKELKNLIPKSAVGTL
SANSSNVIQLIIDAYNSLSSEVILENGKLSEGVTISYKSYCKNGVNGTGENGRKCSNISI
GDEVQFEISITSNKCPKKDSDSFKIRPLGFTEEVEVILQYICECECQSEGIPESPKCHEG
NGTFECGACRCNEGRVGRHCECSTDEVNSEDMDAYCRKENSSEICSNNGECVCGQCVCRK
RDNTNEIYSGKFCECDNFNCDRSNGLICGGNGVCKCRVCECNPNYTGSACDCSLDTSTCE
ASNGQICNGRGICECGVCKCTDPKFQGQTCEMCQTCLGVCAEHKECVQCRAFNKGEKKDT
CTQECSYFNITKVESRDKLPQPVQPDPVSHCKEKDVDDCWFYFTYSVNGNNEVMVHVVEN
PECPTGPDIIPIVAGVVAGIVLIGLALLLIWKLLMIIHDRREFAKFEKEKMNAKWDTGEN
PIYKSAVTTVVNPKYEGK
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BDBM17924
Eu-Labeled Human VCAM-1/Fc Chimera
Name:Eu-Labeled Human VCAM-1/Fc Chimera
Synonyms:Recombinant Human VCAM-1/CD106/Fc Chimera
Type:Other Protein Type
Mol. Mass.:358.43
Organism:n/a
Description:A DNA sequence encoding the signal peptide from human CD33 joined with amino acid residues 25-698 of the extracellular domain of human vascular cell adhesion molecule 1 was fused to the 6X histidine tagged Fc of human IgG1 via a polypeptide linker. The chimeric protein was expressed in a mouse myeloma cell line, NS0.
Residue:3
Sequence:
n/a