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TargetCyclin-A2/Cyclin-dependent kinase 2
LigandBDBM31537
Substrate/CompetitorHistone H1
Meas. Tech.Kinase SPA Assay
pH7.4±n/a
Temperature296.15±n/a K
IC50 574±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-A2/Cyclin-dependent kinase 2
Name:Cyclin-A2/Cyclin-dependent kinase 2
Synonyms:CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A)
Type:Protein Complex
Mol. Mass.:n/a
Description:Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus.
Components:This complex has 2 components.
Component 1
Name:Cyclin-dependent kinase 2
Synonyms:CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (Human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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  Blast E-value cutoff:
Component 2
Name:Cyclin-A2
Synonyms:CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:P20248
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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  Blast E-value cutoff:
BDBM31537
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