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TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1
LigandBDBM6867
Substrate/CompetitorGST-Rb fusion protein
Meas. Tech.Kinase Inhibition Assay
IC50 190±n/a nM
Citation Lin, RConnolly, PJHuang, SWetter, SKLu, YMurray, WVEmanuel, SLGruninger, RHFuentes-Pesquera, ARRugg, CAMiddleton, SAJolliffe, LK 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem48:4208-11 (2005) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Name:Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Synonyms:CDK4/Cyclin D1 | Cyclin-Dependent Kinase 4 (CDK4)
Type:Protein Complex
Mol. Mass.:n/a
Description:The recombinant CDK4/D1 complex was made by co-infecting insect cells with viruses carrying CDK4 and Cyclin D1.
Components:This complex has 2 components.
Component 1
Name:G1/S-specific cyclin-D1
Synonyms:CCND1_MOUSE | Ccnd1 | Cyclin D1 | Cyl-1
Type:Enzyme Subunit
Mol. Mass.:33418.84
Organism:Mus musculus (mouse)
Description:n/a
Residue:295
Sequence:
MEHQLLCCEVETIRRAYPDTNLLNDRVLRAMLKTEETCAPSVSYFKCVQKEIVPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPLKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEADENKQTIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAMQGLNLGSPNNFLSCYRTTHFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNVDPKATEEEGEVEEEAGLACTPTDVRDVDI
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Component 2
Name:Cyclin-dependent kinase 4
Synonyms:CDK4_MOUSE | Cdk4 | Crk3 | cyclin-dependent kinase 4
Type:Enzyme Subunit
Mol. Mass.:33750.96
Organism:Mus musculus (mouse)
Description:n/a
Residue:303
Sequence:
MAATRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGAAGGGLPVSTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDRDIKVTLVFEHIDQDLRTYLDKAPPPGLPVETIKDL
MRQFLSGLDFLHANCIVHRDLKPENILVTSNGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
EVSLPRGAFAPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKEES
DAE
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BDBM6867
GST-Rb fusion protein
Name:GST-Rb fusion protein
Synonyms:Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | RB1 | RB_HUMAN | Rb | retinoblastoma
Type:Other Protein Type
Mol. Mass.:106410.17
Organism:Homo sapiens (Human)
Description:GST-60 kDa Rb fusion protein (comprising amino acids 378 to 928 of retinoblastoma)
Residue:928
Sequence:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSY
RKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
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