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TargetCyclin-Dependent Kinase 2 (CDK2)
LigandBDBM31545
Substrate/CompetitorHistone H1
Meas. Tech.Kinase SPA Assay
IC50 363±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,   Solution Info,  Assay Method
 
Cyclin-Dependent Kinase 2 (CDK2)
Name:Cyclin-Dependent Kinase 2 (CDK2)
Synonyms:CDK2/CycE | CDK2/Cyclin E | CDK2/E | Cyclin-dependent kinase 2/G1/S-specific cyclin E1 | Cyclin-dependent kinase 2/cyclin E1
Type:Protein Complex
Mol. Mass.:n/a
Description:Cdk2/Cyclin E kinase was purified from insect cells coinfected with Cyclin E /Cdk2 baculovirus.
Components:This complex has 2 components.
Component 1
Name:Cyclin-dependent kinase
Synonyms:CDK2 | CDK2-Kinase | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 2
Name:Cyclin E
Synonyms:Cyclin-E | Cyclin-E1 | G1/S-specific cyclin-E1 | Interacts with a member of the CDK2/CDK protein kinases
Type:Enzyme Subunit
Mol. Mass.:47073.17
Organism:Homo sapiens (human)
Description:n/a
Residue:410
Sequence:
MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM31545
Histone H1
Name:Histone H1
Synonyms:n/a
Type:Other Protein Type
Mol. Mass.:358.43
Organism:Bos taurus (bovine)
Description:n/a
Residue:3
Sequence:
n/a