Kinase enzymes - @ a glance

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At a glance

Kinases catalyze the addition of a phosphate group (typically from ATP) to free hydroxyl groups on target molecules, including both proteins and small molecules such as glucose. The negative charge of phosphate groups added during phosphorylation regulates activity, localization and turnover of target proteins. As one of the largest functionally diverse gene families; kinases, through phosphorylation, can regulate signal transduction and essential cellular process including proliferation, apoptosis, differentiation and the cell cycle.

Download the kinome diagram

 

The human genome encodes 518 kinases containing a conserved ATP binding pocket, ~1.7% of all human genes. This includes 478 protein kinases and 40 atypical protein kinases. These protein kinases can be grouped into families based on the sequence of the catalytic domain and species conservation. The seven largest groups of kinases and their relative sequence similarities can be seen in the diagram below. The largest family, tyrosine kinases, phosphorylate target proteins at tyrosine residues; the remaining families primarily target serine and threonine residues.

 

Kinase biochemical products


The kinome pathway

 

ProductBiological descriptionPurityReference
Adenosine Kinase      
Iodotubercidin Potent, adenosine kinase inhibitor >95% Ugarkar et al, 2000
Akt      
SC-66 Allosteric Akt inhibitor >99% Jo et al, 2011
Crosstide Akt peptide substrate >98% Bentley et al, 2007
Crosstide (biotinylated) Akt peptide substrate, biotinylated >98% Cross et al, 1995
AMP-kinase      
SAMS peptide AMP-activated protein kinase substrate >95% Zou et al, 2003
A 769662 AMP-activated protein kinase activator >99% Goransson et al, 2007
AICAR (Acadesine/AICA riboside) Cell-permeable activator of AMP-activated protein kinase >98% Gadalla et al, 2004
Metformin hydrochloride AMPK activator >99% Labuzek et al, 2010
ATM      
KU-55933 Potent, selective and competitive ATM kinase inhibitor >99% Li et al, 2010
CAMK      
K252a Highly potent inhibitor of protein and CAM kinases >99% Kase et al, 1987
KN-62 CaM kinase II inhibitor. P2X7 antagonist. >98% Tokumitsu et al, 1990
Casein kinase      
D4476 CK1 inhibitor >99% Rena et al, 2004
TMCB Selective CK2 inhibitor >98% Pagano et al, 2008
Ellagic acid Selective, casein kinase 2 (CK2) inhibitor >99% Cozza et al, 2006
Cyclin-dependent kinase      
Purvalanol A Potent CDK inhibitor >98% Villerbu et al, 2002
Purvalanol B CDK2 inhibitor >98% Gray et al, 1999
DNA-PK      
NU 7026 Novel, specific, reversible DNA-PK inhibitor >99% Nutley et al, 2005
DYRK      
Harmine Potent and selective inhibitor of DYRK1A >98% Song et al, 2004
General      
H89 dihydrochloride Kinase inhibitor >98% Lochner et al, 2006
Rottlerin Kinase inhibitor >95% Bain et al, 2007
Staurosporine Protein kinase inhibitor >98% Gani et al, 2010
GSK      
Phospho-Glycogen Synthase Peptide-2 GSK substrate >99% Sutherland et al, 1994
SB 216763 Potent selective GSK-3 inhibitor >98% Coghlan et al, 2000
Lithium chloride GSK-3β inhibitor >99% Zhu et al, 2011
JAK      
Nifuroxazide JAK/STAT signaling inhibitor. Nitrofuran antibiotic. >98% Nelson et al, 2008
AG 490 JAK2/3 inhibitor >99% Kirken et al, 1999
MAPK      
JNK      
TCS JNK 5a Selective JNK2/3 inhibitor >99% Angell et al, 2007
SP600125 JNK inhibitor >98% Bennett et al, 2001
MKK/MEK      
SL 327 MEK inhibitor > 9% Wang et al, 2003
PD 98059 MEK1 inhibitor >99% Alessi et al, 1995
U0126 Selective MKK inhibitor >98% Duncia et al, 1998
MNK      
CGP 57380 MNK inhibitor >98% Knauf et al, 2001
p38      
SB 203580 p38 MAP kinase inhibitor >99% Cuenda et al, 2007
SB 203580 hydrochloride p38 MAP kinase inhibitor; water soluble >99% Cuenda et al, 2007
SB 202190 Highly selective, potent, cell permeable p38 MAP kinase inhibitor >99% Karahashi et al, 2000
Raf      
ZM 336372 Potent, selective c-Raf inhibitor >98% Hall-Jackson et al, 1999
PI3K      
Wortmannin PI3-kinase inhibitor >98% Ui et al, 1995
LY 294002 PI3-kinase inhibitor >99% Vlahos et al, 1994
PKA      
cAMP Second messenger. PKA activator. >99% Kazanietz et al, 2000
8-CPT-cAMP Cell permeable cAMP analogue, protein kinase modulator >98% Dieter et al, 1991
PKC      
Phorbol 12-myristate 13-acetate (PMA) PKC activator >99% Kazanietz et al, 2000
Ro 31-8220 mesylate Protein kinase inhibitor >98% Dieter et al, 1991
PKG      
KT5823 Potent, selective inhibitor of PKG >95% Burkhardt et al, 2000
Rho      
Y-27632 dihydrochloride Selective Rho kinase inhibitor >99% Ishizaki et al, 2000
ROCK      
HA-1077 ROCK2 inhibitor >98% Davies et al, 2000
Syk      
Piceatannol Syk tyrosine kinase inhibitor >99% Oliver et al, 1994
Tyrosine kinase      
Genistein Protein tyrosine kinase inhibitor. Anticancer agent. >99% Akiyama et al, 1987
PP1 Potent Src family tyrosine kinase inhibitor >98% Tatton et al, 2003
PP2 Src and RIP2 kinase inhibitor >98% Chong et al, 2005
PP3 Negative control for the Src kinase inhibitor PP2. >98% Hou et al, 2007

References

  1. Graves LM et al. The dynamic nature of the kinome. Biochem J. 450(1):1-8 (2013). Read more (PubMed:23343193) »
  2. Knight JD et al. Profiling the kinome: Current capabilities and future challenges. J Proteomics. (2012). Read more (PubMed:23099349) »
  3. Manning G et al. The protein kinase complement of the human genome. Science. 298(5600):1912-34(2002). Read more (PubMed:12471243) »

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