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TargetCyclin-Dependent Kinase 4 (CDK4)
LigandBDBM31545
Substrate/CompetitorHistidine-tagged Rb
Meas. Tech.Kinase Multiscreen Assay
pH7.4±n/a
Temperature296.15±n/a K
IC50 160±n/a nM
Citation Brasca, MGAmboldi, NBallinari, DCameron, ACasale, ECervi, GColombo, MColotta, FCroci, VD'Alessio, RFiorentini, FIsacchi, AMercurio, CMoretti, WPanzeri, APastori, WPevarello, PQuartieri, FRoletto, FTraquandi, GVianello, PVulpetti, ACiomei, M Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. J Med Chem52:5152-63 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Cyclin-Dependent Kinase 4 (CDK4)
Name:Cyclin-Dependent Kinase 4 (CDK4)
Synonyms:CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/cyclin D1
Type:Protein Complex
Mol. Mass.:n/a
Description:CDK4/D1 complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components.
Components:This complex has 2 components.
Component 1
Name:Cyclin-dependent kinase
Synonyms:CDK4 | Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | Cyclin-dependent kinase 4 (CDK4) | PSK-J3
Type:Enzyme Subunit
Mol. Mass.:33731.96
Organism:Homo sapiens (human)
Description:P11802
Residue:303
Sequence:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL
MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG
NPE
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Component 2
Name:Cyclin-dependent kinase 4/cyclin D
Synonyms:BCL-1 oncogene | Cyclin D1 | Cyclin-D1 | G1/S-specific cyclin D1 | G1/S-specific cyclin-D1 | PRAD1 oncogene | Regulatory component of the cyclin D1-CDK4
Type:Enzyme Subunit
Mol. Mass.:33717.70
Organism:Homo sapiens (human)
Description:n/a
Residue:295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
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BDBM31545
NameBDBM31545
Synonyms:Milciclib | pyrazolo[4,3-h]quinazoline-3-carboxamide, 28
TypeSmall organic molecule
Emp. Form.C25H32N8O
Mol. Mass.460.5746
SMILESCNC(=O)c1nn(C)c-2c1C(C)(C)Cc1cnc(Nc3ccc(cc3)N3CCN(C)CC3)nc-21
Structure
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Histidine-tagged Rb
Name:Histidine-tagged Rb
Synonyms:6x-Histidine tagged truncated form of retinoblastoma (amino acid 386-928) | Rb | Retinoblastoma-associated protein | pRb | pp110 | retinoblastoma
Type:Other Protein Type
Mol. Mass.:106170.80
Organism:Homo sapiens (human)
Description:n/a
Residue:928
Sequence:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIAAVDLDEMSFTFTEL
QKNIEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDARLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNVIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
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