Kinase Profiling & HTS

kinase gold standard

 

Kinase Hotspot SM

Pharma labs typically only use P33 radiolabeled kinase assay profiling for only a few select compounds. Now, RBC's proprietary nanoliter screening techniques make this gold standard kinase assay format available for large-scale profiling and HTS. Now you can get radioisotope data for a fluorescent price. Read the Expert Opinion review on the challenge of selecting protein kinase assays for lead discovery optimization.

 

Benefits of Kinase HotSpot SM include:

  • Gold Standard radiolabeled data: Avoid the false negatives and positives that are generated by fluorescent assay formats;

  • 341 kinase assays available, and growing;

  • Costs can be as low as outsourced fluorescent screens;

  • HotSpot's low cost lets you profile more compounds earlier, and avoid dead-end leads;

  • HotSpot HTS brings economic radiolabeled assaying to HTS: Shorten your hit validation timeline;

  • Flexible ATP concentration from 1µM to 10µM can be used. Low 1µM ATP concentration means that ATP competitive inhibitors are easier to spot.

Kinase HotSpot SM screens are available in:

Kinase Assay Type
Sample Price*
HTS — 1 kinase $3.00 / well:
20,000 compound order
10 dose IC50 vs 50
kinase assay panel
$50 / IC50:
20 compounds
10 dose IC50 vs 100
kinase assay panel
$40 / IC50:
20 compounds
10 dose IC50 vs 200
kinase assay panel
$30 / IC50:
20 compounds

* The price is subject to change and discounts may apply for larger orders. Please call 1-877-347-2368 or 1-610-722-0247 for details.

 

Kinase Assay Services Available:

  • Larger scale HTS;

  • Large scale single dose, duplicate profiling;

  • IC50 profiling — 5 or 10 dose with curve fitting;

  • ATP — competitive evaluation;

  • Compound binding reversibility test;

  • Ki determination;

  • Custom Assay development;

  • Substrate determination;

  • Research collaboration.

RBC can quote any subset of its 341 kinase availability. Pricing is subject to change without notice. Mutant panel pricing available by quotation only. Custom assay development for customer-supplied kinases is also available. RBC's nanoliter screening can help make expensive assays with problem kinases more economical.

For more information on Kinase HotSpot SM, or for a free price quote, call 1-877-347-2368 or 1-610-722-0247 or email sales@reactionbiology.com.


HotSpot Image with Resulting Data


Z' Factor, c-Src Assay


IC50 Values (nM) of Staurosporine Profiled Against 50 Kinases


Reproducibility: Actual HTS Run

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Receptor Tyrosine Kinases
ALK EPHB2 IRR/INSRR
AXL EPHB3 KDR/VEGFR2
c-KIT EPHB4 MUSK
c-MER ERBB2/HER2 PDGFRa 
c-MET ERBB4/HER4 PDGFRb 
DDR2 FGFR1 RET
EGFR FGFR2 RON/MST1R
EPHA1 FGFR3 ROS/ROS1
EPHA2 FGFR4 TIE2/TEK
EPHA3 FLT1/VEGFR1 TRKA
EPHA4 FLT3 TRKB
EPHA5 FLT4/VEGFR3 TRKC
EPHA6    
EPHA7 FMS TYK1/LTK
EPHA8 IGF1R TYRO3_SKY
EPHB1 IR  

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RAF/MEK/ERK Pathway Kinases
AKT1 MEK2 PI3Kg (p120g)
AKT2 MLK1/MAP3K9 PKA
AKT3 MLK2/MAP3K10 PKAcg
ARAF MLK3/MAP3K11 PKCa
  MNK1 PKCb1
BRAF MNK2 PKCb2
COT1/MAP3K8 P70S6K/RPS6KB1 PKCd
c-SRC PAK1 PKCepsilon
ERK1/MAPK3 PAK2 PKCeta
ERK2/MAPK1 PAK3 PKCg
FAK/PTK2 PAK4 PKCiota
LYN PAK5 PKCmu/PRKD1
MAPKAPK2 PAK6 PK theta
MAPKAPK3 PI3Ka (p110a/p85a) PKCzeta
MAPKAPK5/PRAK PI3Kb(p110b/p85a) PYK2
MEK1 PI3Kd (p110d/p85a) RAF1
RAF/MEK/ERK Pathway

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PI3K-AKT Pathway Kinases
AKT1 DNA-PK  
AKT2 ERK1/MAPK3  
AKT3 ERK2/MAPK1 PDK1/PDPK1
ARAF GSK3a PI3Ka (p110a/p85a)
ASK1/MAP3K5 GSK3b PI3Ka (p110b/p85a)
BRAF IKKa/CHUK PI3Ka (p110d/p85a)
CHK1 IKK/IKBKB PI3Kg (p120g)
CHK2 mTOR/FRAP1 RAF1
COT1/MAP3K8 P70S6K/RPS6KB1  
PI3K/AKT Pathway

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Oncology Kinases
ABL1 EPHB2 MRCKb/
CDC42BPB
ABL2/ARG EPHB3 MST4
AKT1 EPHB4 MUSK
AKT2 ErbB2/HER2 NEK1
AKT3 ErbB4/HER4 P38a/MAPK14
Aurora A FAK/PTK2 P38b/MAPK11
Aurora B FER P38d/MAPK13
Aurora C FES/FPS P38g/MAPK12
AXL FGFR1 P70S6K/RPS6KB1
BRAF FGFR2 PAK4
BRK FGFR3 PDGFRa
BTK FGFR4 PDGFRb
CDK1/cyclin B FGR PI3Ka
(p110a/p85a)
CDK2/cyclin A FLT1/VEGFR1 PI3Kb
(p110b/p85a)
CDK4-cyclin D1 FLT3 PI3Kd
(p110d/p85a)
CDK5/p25 FLT4/VEGFR3 PI3Kg(p120g)
CDK6/cyclin D1 FMS PIM1
CDK7/cyclin H FYN PIM2
CDK9/Cyclin T1 HCK PKCa
CHK1 HGK/MAP4K4 PKCb1
CHK2 HIPK1 PKCd
CK1epsilon HIPK2 PK epsilon
CK2a HIPK3 PKCeta
c-KIT HIPK4 PKCtheta
c-MET IGF1R PLK1
COT1/MAP3K8 IKKa/CHUK PYK2
c-SRC IKK/IKBKB RAF1
CTK/MATK JAK1 RET
DAPK1 JAK2 ROCK1
DNA-PK JAK3 RON/MST1R
EEF2K JNK1 ROS/ROS1
EGFR JNK2 SGK1
EPHA1 JNK3 SYK
EPHA2 KDR/VEGFR2 TGFBR2
EPHA3 LCK TIE2?TEK
EPHB4 LKB1 TRKA
EPHA5 LYN TRKB
EPHA6    
EPHA7 MEK1 TRKC
EPHA8 MEK2 TYRO3/SKY
EPHB1 MRCKa/
CDC42BPA
YES/YES1

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Exploration Kinases
ABL1 ERK2/MAPK1 P38a/MAPK14
AKT1 FGFR1 PAK1
Aurora A FGFR2 PAK2
BTK FGFR3 PDGFRa
CAMKIIb FLT1/VEGFR1 PHKg2
CDK1/cyclin B FLT3 PIM1
CDK2/cyclin A FLT4/VEGFR3 PKA
CHK1 GSK3b PKCa
CHK2 HIPK1 PLK2
c-MET IR RET
c-SRC IRAK4 ROCK1
DAPK1 JAK3 RSK1
EGFR KDR/VEGFR2 SYK
EPHA3 LCK TAK1
EPHB4 LYN TIE2?TEK
ErbB4/HER4 MINK/MINK1 TRKA
ERK1/MAPK3 MST2/STK3  

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Special Kinases
AMPK(A1/B1/G1) EEF2K PDK4/PDHK4
AMPK(A1/B1/G2) EIF2AK1 PI3Ka
(p110a/p85a)
AMPK(A1/B1/G3) EIF2AK2 PI3Kb
(p110b/p85a)
AMPK(A1/B2/G1) EIF2AK3 PI3Kd
(p110d/p85a)
AMPK(A2/B1/G1)   PI3Kg(p120g)
DNA-PK mTOR/FRAP1  

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KINOME MAPPING APP. DISPLAY YOUR SCREENING RESULTS WITH RBC'S FREE APPLICATION HERE


kinases

Kinases (Kinase Mutants below)

(Click on names for PDFs)

A.  Human Kinome Kinases

SPECIAL PRODUCT PANELS:
B.  Receptor Tyrosine Kinases — indicated in pink (also see complete list)
C.  RAF/MEK/ERK Pathway Kinases — indicated in blue (also see complete list and diagram)
D.  PI3K-AKT Pathway Kinases — indicated in yellow (also see complete list and diagram)
E.  Oncology Kinases — indicated in green (also see complete list)
F.  Exploration Kinases — indicated in red (also see complete list)
G.  Special Kinases — indicated in purple (also see complete list)

Kinase A B C D E F G
ABL1 x       x x  
ABL2/ARG x       x    
ACK1              
AKT1 x   x x x x  
AKT2 x   x x x    
AKT3 x   x x x    
ALK x x          
ALK1/ACVRL1              
ALK2/ACVR1              
ALK4/ACVR1B x            
ALK5/TGFBR1 x            
AMPK(A1/B1/G1)             x
AMPK(A1/B1/G2)             x
AMPK(A1/B1/G3)             x
AMPK(A1/B2/G1)             x
AMPK(A2/B1/G1)             x
ARAF x   x x      
ARK5/NUAK1 x            
ASK1/MAP3K5 x     x      
Aurora A x       x x  
Aurora B x       x    
Aurora C x       x    
AXL x x     x    
BLK x            
BMX/ETK x            
BRAF x   x x x    
BRK x       x    
BRSK1 x            
BRSK2 x            
BTK x       x x  
CAMK1a x            
CAMK1b x            
CAMK1d x            
CAMK1g x            
CAMKIIa x            
CAMKIIb x         x  
CAMKIId x            
CAMKIIg x            
CAMK4 x            
CAMKK1 x            
CAMKK2 x            
CDK1/cyclin A              
CDK1/cyclin B x       x x  
CDK2/cyclin A x       x x  
CDK2/cyclin E x            
CDK3/cyclin E x            
CDK4-cyclin D1 x       x    
CDK4/cyclin D3              
CDK5/p25 x       x    
CDK5/p35 x            
CDK6/cyclin D1 x       x    
CDK6/cyclin D3 x            
CDK7/cyclin H x       x    
CDK9/Cyclin K x            
CDK9/Cyclin T1 x       x    
CHK1 x     x x x  
CHK2 x     x x x  
CK1a1 x            
CK1d x            
CK1epsilon x       x    
CK1g1 x            
CK1g2 x            
CK1g3 x            
CK2a x       x    
CK2a2 x            
c-KIT x x     x    
CLK1 x            
CLK2 x            
CLK3 x            
CLK4 x            
c-MER x x          
c-MET x x     x x  
COT1/MAP3K8 x   x x x    
CSK x            
c-SRC x   x   x x  
CTK/MATK x       x    
DAPK1 x       x x  
DAPK2 x            
DCAMKL2 x            
DDR2 x x          
DMPK x            
DNA-PK       x x   x
DRAK1/STK17A x            
DYRK1/DYRK1A x            
DYRK1B x            
DYRK2 x            
DYRK3 x            
DYRK4 x            
EEF2K         x   x
EGFR x x     x x  
EIF2AK1             x
EIF2AK2             x
EIF2AK3             x
EPHA1 x x     x    
EPHA2 x x     x    
EPHA3 x x     x x  
EPHA4 x x     x    
EPHA5 x x     x    
EPHA6 x x     x    
EPHA7 x x     x    
EPHA8 x x     x    
EPHB1 x x     x    
EPHB2 x x     x    
EPHB3 x x     x    
EPHB4 x x     x x  
ERBB2/HER2 x x     x    
ERBB4/HER4 x x     x x  
ERK1/MAPK3 x   x x   x  
ERK2/MAPK1 x   x x   x  
FAK/PTK2 x   x   x    
FER x       x    
FES/FPS x       x    
FGFR1 x x     x x  
FGFR2 x x     x x  
FGFR3 x x     x x  
FGFR4 x x     x    
FGR x       x    
FLT1/VEGFR1 x x     x x  
FLT3 x x     x x  
FLT4/VEGFR3 x x     x x  
FMS x x     x    
FRK/PTK5 x            
FYN x       x    
GCK/MAP4K2 x            
GRK2 x            
GRK3 x            
GRK4 x            
GRK5 x            
GRK6 x            
GRK7 x            
GSK3a x     x      
GSK3b x     x   x  
Haspin x            
HCK x       x    
HGK/MAP4K4 x       x    
HIPK1 x       x x  
HIPK2 x       x    
HIPK3 x       x    
HIPK4 x       x    
IGF1R x x     x    
IKKa/CHUK x     x x    
IKKb/IKBKB x     x x    
IKKe/IKBKE x            
IR x x       x  
IRAK1 x            
IRAK4 x         x  
IRR/INSRR x x          
ITK x            
JAK1 x       x    
JAK2 x       x    
JAK3 x       x x  
JNK1 x       x    
JNK2 x       x    
JNK3 x       x    
KDR/VEGFR2 x x     x x  
KHS/MAP4K5              
LCK x       x x  
LKB1 x       x    
LIMK1 x            
LOK/STK10 x            
LRRK2 x            
LYN x   x   x x  
LYNB x            
MAPKAPK2 x   x        
MAPKAPK3 x   x        
MAPKAPK5/PRAK x   x        
MARK1 x            
MARK2/PAR-1Ba x            
MARK3 x            
MARK4              
MEK1 x   x   x    
MEK2 x   x   x    
MEKK2 x            
MEKK3 x            
MELK x            
MINK/MINK1 x         x  
MKK6              
MLCK/MYLK x            
MLCK2/MYLK2 x            
MLK1/MAP3K9 x   x        
MLK2/MAP3K10 x   x        
MLK3/MAP3K11 x   x        
MNK1 x   x        
MNK2 x   x        
MRCKa/
CDC42BPA
x       x    
MRCKb/
CDC42BPB
x       x    
MSK1/RPS6KA5 x            
MSK2/RPS6KA4 x            
MSSK1/STK23 x            
MST1/STK4 x            
MST2/STK3 x         x  
MST3/STK24 x            
MST4 x       x    
mTOR/FRAP1       x     x
MUSK x x     x    
MYO3b x            
NEK1 x       x    
NEK2 x            
NEK3 x            
NEK4 x            
NEK6 x            
NEK7 x            
NEK9 x            
NEK11 x            
NIK/MAP3K14 x            
NLK x            
OSR1/OXSR1 x            
P38a/MAPK14 x       x x  
P38b/MAPK11 x       x    
P38d/MAPK13 x       x    
P38g/MAPK12 x       x    
P70S6K/RPS6KB1 x   x x x    
p70S6Kb/
RPS6KB2
x            
PAK1 x   x     x  
PAK2 x   x     x  
PAK3 x   x        
PAK4 x   x   x    
PAK5 x   x        
PAK6 x   x        
PASK x            
PBK/TOPK x            
PDGFRa x x     x x  
PDGFRb x x     x    
PDK1/PDPK1 x     x      
PDK4/PDHK4             x
PHKg1              
PHKg2 x         x  
PI3Ka
(p110a/p85a)
    x x x   x
PI3Kb
(p110b/p85a)
    x x x   x
PI3Kd
(p110d/p85a)
    x x x   x
PI3Kg(p120g)     x x x   x
PIM1 x       x x  
PIM2 x       x    
PIM3 x            
PKA x   x     x  
PKAcg x   x        
PKCa x   x   x x  
PKCb1 x   x   x    
PKCb2 x   x        
PKCd x   x   x    
PKCepsilon x   x   x    
PKCeta x   x   x    
PKCg x   x        
PKCiota x   x        
PKCmu/PRKD1 x   x        
PKCnu/PRKD3 x            
PKCtheta x   x   x    
PKCzeta x   x        
PKD2/PRKD2 x            
PKG1a x            
PKG1b x            
PKG2/PRKG2 x            
PKN1/PRK1 x            
PKN2/PRK2 x            
PLK1 x       x    
PLK2 x         x  
PLK3 x            
PRKX x            
PYK2 x   x   x    
RAF1 x   x x x    
RET x x     x x  
RIPK2 x            
RIPK5              
ROCK1 x       x x  
ROCK2 x            
RON/MST1R x x     x    
ROS/ROS1 x x     x    
RSK1 x         x  
RSK2 x            
RSK3 x            
RSK4 x            
SGK1 x       x    
SGK2 x            
SGK3/SGKL x            
SIK2 x            
SLK/STK2              
SNARK/NUAK2 x            
SRMS              
STK16              
STK22D/TSSK1 x            
STK25/YSK1              
STK33 x            
STK38/NDR1 x            
STK39/STLK3 x            
SRPK1 x            
SRPK2 x            
SYK x       x x  
TAK1 x         x  
TAOK1 x            
TAOK2/TAO1 x            
TAOK3/JIK x            
TBK1 x            
TEC x            
TGFBR2 x       x    
TIE2/TEK x x     x x  
TLK2 x            
TRKA x x     x x  
TRKB x x     x    
TRKC x x     x    
TSSK2 x            
TTK x            
TXK x            
TYK1/LTK x x          
TYK2 x            
TYRO3/SKY x x     x    
ULK1 x            
ULK2 x            
ULK3 x            
VRK1 x            
WEE1 x            
WNK2 x            
WNK3 x            
YES/YES1 x       x    
ZAK/MLTK x            
ZAP70 x            
ZIPK/DAPK3 x            
KINASE
MUTANTS
             
ABL1(E255K)              
ABL1(G250E)              
ABL1(H396P)              
ABL1(M351T)              
ABL1(Q252H)              
ABL1(T315I)              
ABL1(Y253F)              
BRAF(V599E)              
BTK(E41K)              
CHK2(I157T)              
c-KIT(D816H)              
c-KIT(D816V)              
C-Kit (T670I)              
C-Kit (V560G)              
c-KIT(V654A)              
c-MET(M1250T)              
c-Src(T341M)              
EGFR(L858R)              
EGFR(L861Q)              
EGFR(T790M)              
EGFR
(L858R,T790M)
             
FGFR1(V561M)              
FGFR2(N549H)              
FGFR3(K650E)              
FLT3(D835Y)              
JAK2 (V617F)              
LRRK2 (D1994A)              
LRRK2 (R1441C)              
LRRK2 (G2019S)              
LRRK2 (I2020T)              
p38a(T106M)              
PDGFRa(D842V)              
PDGFRa(T674I)              
PDGFRa(V561D)              
RET(V804L)              
RET(V804M)              

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