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Comprehensive Kinome Coverage

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TK CAMK CGMC AGC STE
TKL CK1 RCG Atypical Other

 

TK TK Tyrosine Kinase
88/91 (97%)
Key Members ABL1, EGFR, HER2, FGFR1, JAK1, c-KIT, SRC
Chemical Inhibitors AG-1478, AG-1517, AG-879, Apigenin, Genistein, Src I1, Lestaurtinib

 

 

 

 

 

HER2 and EGFR are receptor tyrosine kinases (RTKs), which have well defined roles in lung and breast cancer. These kinases normally initiate multiple downstream signaling pathways. Given their pivotal roles in activating multiple signaling events, hyperactivation or overexpression of HER2 and EGFR lead to HER2-positive breast cancer and non-small cell lung cancer (NSCLC) respectively. Fortunately, their cell-surface localization at the makes RTKs amenable to pharmaceutical intervention by monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs).

CAMK CAMK Calmodulin/Calcium Regulated Kinase
67/74 (91%)
Key Members AMPK α1, CaMK1, CHK1, DAPK1
Chemical Inhibitors Dorsomorphin, BML-277

 

 

 

 

 

CAMKs mediate many of the second messenger effects of Ca2+. AMPK and CAMK2 are members of the CAMK family that are implicated in metabolic disease, cancer, learning and heart disease. AMPK is a metabolic regulator that is activated when ATP levels are low. Interestingly, the incidence of cancer is reduced in Type 2 diabetes patients who are treated with treated with metformin, an AMPK activator – providing an opportunity for cancer prevention and therapy. CAMK2 plays a part in integrating short-term and long-term memories and is therefore called the “memory molecule”. CAMK2 is also promotes contractile strength of cardiac muscle and too much signaling through this kinase results in high blood pressure and cardiac hypertrophy.

TK CMGC CDK, MAPK, GSK3 and CLK 
59/63 (94%)
Key Members ERK1, p38α, CDK1, HIPK1, JNK1
Chemical Inhibitors Doramapimod, JX-401, Alsterpaullone, SP-600125

 

 

 

 

 

CMGC kinases preferentially phosphorylate proline-rich target sequences. Because of their essential role in cell cycle regulation, CDKs are amongst the most studied members of the CGMC family. Dysregulated CDK function gives rise to abnormal cell growth, which leads to cancers. Efforts to target CDKs in cancer therapy have revealed that these enzymes can compensate for one another, leading to little or no effect when inhibiting a single kinase. Current strategies involve designing inhibitors that are effective against multiple CDKs to address this issue.

AGC AGC Protein Kinase A, G, and C
57/63 (90%)
Key Members AKT, P70S6K, PKAc, PKCa, PKN1, SGK1
Chemical Inhibitors Deguelin, NPC-15437, LYS6K2

 

 

 

 

 

AGC kinases are categorized based upon similarities in their kinase domains. PDK1 is an AGC kinase, which is required for phosphorylating many of its fellow AGC members. One of its substrates is AKT1/PKBα, a central node in cell signaling for growth factors, cytokines, and other stimuli. AKT1 turns on programs for cell survival and proliferation, a property that also promotes tumor cell survival and resistance to apoptosis. AKT1 remains an elusive target for inhibition because other AGC kinases are able to compensate when AKT1 function is lost.

STE STE Homologs of the yeast STE7, STE11 and STE20
57/63 (90%)
Key Members ASK1, MEK1, MEKK1, PAK1, HPK1, TAOK1, MST1
Chemical Inhibitors PD-98059

 

 

 

 

 

STE kinases are named after the yeast sterile20 (Ste20) ser/thr kinase. The STE subfamily includes many enzymes involved in MAP kinase signaling, including the mammalian Ste20-like kinases (MSTs). There are five MSTs in humans: MST1 (STK4), MST2 (STK3), MST3 (STK24), MST4 (STK26), and YSK1 (STK25). MSTs 1 and 2 are potent activators of cell proliferation and MSTs 3 and 4 regulate cytoskeletal control and cell migration. Not surprisingly, mutations and fusions of MSTs have been observed in cancers. Aberrant MSTs 1 and 2 are connected to the rare cancer, mesothelioma and MSTs 3 and 4 promote metastasis in aggressive breast cancer subtypes.

TKL TKL Tyrosine Kinase-Like
40/45 (89%)
Key Members ALK1, BRAF, IRAK1, LRRK2, MLK1, RIPK1, TGFBR1
Chemical Inhibitors GW-5074, Sorafenib, ZM-336372

 

 

 

 

 

The TKL subfamily is a divergent group of kinases, which share sequence similarity to the TKs. TKL is divided into several subgroups, including the IL1 Receptor Associated Kinases (IRAKs) and Receptor Interacting Protein Kinases (RIPKs). As effectors of Toll-like receptors (TLRs), IRAKs and RIPKs activate innate and active immune responses. IRAK4 deficiency provides protection from developing rheumatoid arthritis (RA), prompting the development of drugs IRAK4-targeted drugs to treat autoimmune diseases. RIPKs 1 and 3 are instrumental inhibiting and triggering necroptosis, a form of cell death that causes leakage of cellular contents. Products of necroptosis are ligands for TLRs; thus, driving a feed-forward mechanism that promotes inflammation.

CK1 CK1 Casein Kinase 1
12/12 (100%)
Key Members CK1alpha1, CK1gamma1
Chemical Inhibitors Staurosporine

 

 

 

 

 

The CK1 group of ser/thr kinases regulate cell differentiation, proliferation, cytoskeleton dynamics, chromosomal segregation, DNA repair and circadian rhythms. CK1 has seven isoforms and these are localized to various intracellular regions including the nucleus, where it directly interacts with the mitotic spindle to regulate the cell cycle.  CK1 α, δ, and ε activate the tumor suppressor p53 to ensure centrosome integrity and genomic stability. Dysregulation or deletion of CK1 isoforms leads to neurodegenerative diseases and many types of cancers.

RGC RGC Receptor Guanylate Cyclases
2/5 (40%)
Key Members NPR1, NPR2
Chemical Inhibitors n/a

 

 

 

 

 

RGC kinases are single-pass transmembrane receptors that have a guanylate cyclase enzyme domain and an inactive protein kinase-like domain. The RGC kinases NPR1 and NPR2 serve as the receptors for BNP and ANP, ligands that are secreted during periods of cardiac stress. Not surprisingly, ANP and BNP levels are established biomarkers for cardiovascular diseases. NPR1/2 signaling regulates blood pressure by mitigating the effects of excess water, sodium and fat. Recently, NPR1 has been implicated in the development of cancer via its role in promoting angiogenesis recruiting stem cells.

Atypical Atypical
20/40 (55%)
Key Members ADCK1, ATM, ATR, BCR, PTK9, TAF1
Chemical Inhibitors n/a

 

 

 

 

 

Eukaryotic Protein Kinases (ePKs) represent the majority of kinases in humans. The atypical kinases are so-named because their catalytic domains lack similarity to those of ePKs. There are several medically relevant atypical kinases, such as BCR and the PDHKs. The constitutively active kinase BCR-ABL is found in the vast majority of chronic myelogenous leukemia (CML) patients, providing the rationale for producing TKIs against BCR-ABL and mutant variants of the fusion protein that provide secondary resistance. PDHKs regulate mitochondrial metabolism by inhibiting the Krebs cycle, which makes PDHK an excellent target for managing metabolic diseases, such as diabetes.

Other Other 
189/105 (85%)
Key Members AURORA AIKKalphaNEK1PI3K (p110 alpha)RIOK1WNK1
Chemical Inhibitors PKC-412PX-866LY-294002STO-609

 

 

 

 

 

There are many kinases that cannot be classified within the conventional subfamilies. These “other” kinases include notable groups, such as the aurora kinases. There are three aurora kinases in humans and they are essential for regulating various aspects of mitosis, including: checkpoint monitoring, spindle assembly, centrosome alignment and cytokinesis. Dysregulation of aurora kinases results in mitosis-related defects, including cells that are aneuploid, polyploid or multinucleate. With their implications in chromosomal instability, aurora kinases are being targeted for the treatment of solid and hematological cancers.

 

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Product Types
Enzymes
Enzymes Active AcetyltransferasesActive Acetyltransferases
Enzymes Active Arginine DeiminasesActive Arginine Deiminases
Enzymes Active Histone DeacetylasesActive Histone Deacetylases
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Antibodies
Antibodies Isoform Specific AntibodiesIsoform Specific Antibodies
Antibodies Modification AntibodiesModification Antibodies
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Antibodies Secondary AntibodiesSecondary Antibodies
Antibodies Tag AntibodiesTag Antibodies
Biochemical Compounds
Biochemical Compounds Epigenetic Enzyme ActivatorsEpigenetic Enzyme Activators
Biochemical Compounds Epigenetic Enzyme InhibitorsEpigenetic Enzyme Inhibitors
Biochemical Compounds Kinase ActivatorsKinase Activators
Biochemical Compounds Kinase InhibitorsKinase Inhibitors
Biochemical Compounds Phosphatase InhibitorsPhosphatase Inhibitors
Biochemical Compounds siRNA ControlssiRNA Controls
Biochemical Compounds siRNA SetssiRNA Sets
Signaling Proteins
Signaling Proteins Acetyl/MethyltransferasesAcetyl/Methyltransferases
Signaling Proteins Adaptor ProteinsAdaptor Proteins
Signaling Proteins Apoptosis ProteinsApoptosis Proteins
Signaling Proteins Arginine DeiminasesArginine Deiminases
Signaling Proteins Cell Cycle ProteinsCell Cycle Proteins
Signaling Proteins Cell Stress & Chaperone ProteinsCell Stress & Chaperone Proteins
Signaling Proteins Cellular ProteinsCellular Proteins
Signaling Proteins Deacetylase/DemethylasesDeacetylase/Demethylases
Signaling Proteins DioxygenasesDioxygenases
Signaling Proteins Fructose KinasesFructose Kinases
Signaling Proteins G-ProteinsG-Proteins
Signaling Proteins Kinase ProteinKinase Protein
Signaling Proteins Lysyl OxidasesLysyl Oxidases
Signaling Proteins Microtubule/Actin Associated ProteinsMicrotubule/Actin Associated Proteins
Signaling Proteins Tau ProteinsTau Proteins
Signaling Proteins Transcription ProteinsTranscription Proteins
Signaling Proteins Ubiquitin ProteinsUbiquitin Proteins
Signaling Proteins Unactive KinasesUnactive Kinases
Signaling Reagents
Signaling Reagents Assay ReagentsAssay Reagents
Signaling Reagents Oligo SubstratesOligo Substrates
Signaling Reagents Peptide SubstratesPeptide Substrates
Signaling Reagents Protein SubstratesProtein Substrates
Extracellular Ligands
Extracellular Ligands ChemokinesChemokines
Extracellular Ligands CytokinesCytokines
Extracellular Ligands Growth FactorsGrowth Factors
Discovery Services
Compound Selective ProfilingCompound Selective Profiling
Custom Protein DevelopmentCustom Protein Development

Research Categories
AKT/PKB PathwayAKT/PKB Pathway
AngiogenesisAngiogenesis
Apoptosis/AutophagyApoptosis/Autophagy
CancerCancer
Cardiovascular DiseaseCardiovascular Disease
Cell CycleCell Cycle
Cellular StressCellular Stress
Cytoplasmic Tyrosine KinasesCytoplasmic Tyrosine Kinases
ERK/MAPK PathwayERK/MAPK Pathway
InflammationInflammation
Invasion/MetastasisInvasion/Metastasis
JAK/STAT PathwayJAK/STAT Pathway
JNK/SAPK PathwayJNK/SAPK Pathway
Lipid KinasesLipid Kinases
Metabolic DisorderMetabolic Disorder
NeurobiologyNeurobiology
NfkB PathwayNfkB Pathway
p38 Pathwayp38 Pathway
PhosphatasesPhosphatases
PhosphodiesterasesPhosphodiesterases
PKA/PKC PathwayPKA/PKC Pathway
Receptor Tyrosine KinasesReceptor Tyrosine Kinases
Ser/Thr KinasesSer/Thr Kinases
WNT SignalingWNT Signaling
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