Kinase Profiling & HTS

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;
K_i 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

Receptor Tyrosine Kinases
ALK	EPHB2	IRR
AXL	EPHB3	KDR/VEGFR-2
c-KIT	EPHB4	MUSK
c-MER	ErbB2/HER2	PDGFR alpha
c-MET	ErbB4/HER4	PDGFR beta
DDR2	FGFR1	RET
EGFR	FGFR2	RON
EPHA1	FGFR3	ROS
EPHA2	FGFR4	TIE2
EPHA3	FLT1/VEGFR-1	TRKA
EPHA4	FLT3	TRKB
EPHA5	FLT4	TRKC
EPHA7	FMS	TYK1/LTK
EPHA8	IGF1R	TYRO3_SKY
EPHB1	IR

RAF/MEK/ERK Pathway Kinases
AKT1	MEK2	PI3Kg (p120g)
AKT2	MLK1	PKA
AKT3	MLK2	PKC alpha
ARAF	MLK3	PKC beta1
BRAF	MNK2	PKC beta2
COT1/MAP3K8	P70s6k	PKC delta
c-SRC	PAK1	PKC epsilon
ERK1	PAK2	PKC eta
ERK2	PAK3	PKC gamma
FAK	PAK4	PKC iota
LYN	PAK5	PKC mu
MAPKAPK2	PAK6	PKC theta
MAPKAPK3	PI3Ka (p110a/p85a)	PKCzeta(PKCz)
MAPKAPK5/PRAK	PI3Kb(p110b/p85a)	PYK2
MEK1	PI3Kd (p110d/p85a)	RAF1

PI3K-AKT Pathway Kinases
AKT1	DNA-PK
AKT2	ERK1
AKT3	ERK2	PDPK1
ARAF	GSK3a	PI3Ka (p110a/p85a)
ASK1	GSK3B	PI3Ka (p110b/p85a)
BRAF	IKK alpha	PI3Ka (p110d/p85a)
CHK1	IKK beta	PI3Kg (p120g)
CHK2	mTOR	RAF1
COT1/MAP3K8	P70s6k

Oncology Kinases
ABL1	EPHB2	MRCKB/ CDC42BPB
ABL2/ARG	EPHB3	MST4
AKT1	EPHB4	MUSK
AKT2	ErbB2/HER2	NEK1
AKT3	ErbB4/HER4	P38 alpha
Aurora A	FAK	P38 beta
Aurora B	FER	P38 delta
Aurora C	FES/FPS	P38 gamma
AXL	FGFR1	P70s6k
BRAF	FGFR2	PAK4
BRK	FGFR3	PDGFR alpha
BTK	FGFR4	PDGFR beta
CDK1/cyclinB	FGR	PI3Ka (p110a/p85a)
CDK2/cyclinA	FLT1/VEGFR-1	PI3Kb (p110b/p85a)
CDK4-cyclinD1	FLT3	PI3Kd (p110d/p85a)
CDK5/p25	FLT4	PI3Kg(p120g)
CDK6/cyclinD1	FMS	PIM1
CDK7/cyclin H/MNAT1	FYN	PIM2
CDK9/CyclinT1	HCK	PKC alpha
CHK1	HGK/MAP4K4	PKC beta1
CHK2	HIPK1	PKC delta
CK1e	HIPK2	PKC epsilon
CK2 alpha	HIPK3	PKC eta
c-KIT	HIPK4	PKCtheta
c-MET	IGF1R	PLK1
COT1/MAP3K8	IKK alpha	PYK2
c-SRC	IKK beta	RAF1
CTK/MATK/HYL	JAK1	RET
DAPK1	JAK2	ROCK1
DNA-PK	JAK3	RON
EEF2K	JNK1 alpha 1	ROS
EGFR	JNK2	SGK1
EPHA1	JNK3	SYK
EPHA2	KDR/VEGFR-2	TGFbR2
EPHA3	LCK	TIE2
EPHB4	LKB1 (STK11)	TRKA
EPHA5	LYN	TRKB
EPHA7	MEK1	TRKC
EPHA8	MEK2	TYRO3_SKY
EPHB1	MRCKA/ CDC42BPA	YES

Exploration Kinases
ABL1	ERK2	P38 alpha
AKT1	FGFR1	PAK1
Aurora A	FGFR2	PAK2
BTK	FGFR3	PDGFR alpha
CAMKIIb beta	FLT1/VEGFR-1	PHK gamma2
CDK1/cyclinB	FLT3	PIM1
CDK2/cyclinA	FLT4	PKA
CHK1	GSK3B	PKC alpha
CHK2	HIPK1	PLK2
c-MET	IR	RET
c-SRC	IRAK4	ROCK1
DAPK1	JAK3	RSK1
EGFR	KDR/VEGFR-2	SYK
EPHA3	LCK	TAK1
EPHB4	LYN	TIE2
ErbB4/HER4	MINK	TRKA
ERK1	MST2

Special Kinases
AMPK(A1/B1/G1)	EEF2K	PDK4
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)	FGFR2	PI3Kg(p120g)
DNA-PK	mTOR

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/TNK2
AKT1	x		x	x	x	x
AKT2	x		x	x	x
AKT3	x		x	x	x
ALK	x	x
ALK1/ACVRL1
ALK2/ACVR1
ALK4	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	x
ASK1	x			x
Aurora A	x				x	x
Aurora B	x				x
Aurora C	x				x
AXL	x	x			x
BLK	x
BMX	x
BRAF	x		x	x	x
BRK	x				x
BRSK1	x
BRSK2	x
BTK	x				x	x
CAMK1a alpha	x
CAMK1b	x
CAMK1d	x
CAMK1g	x
CAMKIIa alpha	x
CAMKIIb beta	x					x
CAMKIId delta	x
CAMKIIg gamma	x
CAMK4	x
CAMKK1	x
CAMKK2	x
CDK1/cyclin A2
CDK1/cyclinB	x				x	x
CDK2/cyclinA	x				x	x
CDK2/cyclinE	x
CDK3/cyclinE	x
CDK4-cyclinD1	x				x
CDK4/cyclinD3
CDK5/p25	x				x
CDK5/p35	x
CDK6/cyclinD1	x				x
CDK6/cyclinD3	x
CDK7/cyclin H/MNAT1	x				x
CDK9/CyclinK	x
CDK9/CyclinT1	x				x
CHK1	x			x	x	x
CHK2	x			x	x	x
CK1a1 alpha	x
CK1d	x
CK1e	x				x
CK1g1/CSNK1G1	x
CK1g2	x
CK1g3/CSNK1G3	x
CK2 alpha	x				x
CK2a2	x
c-KIT	x	x			x
CLK1 CD	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/HYL	x				x
DAPK1	x				x	x
DAPK2	x
DCAMKL2	x
DDR2	x	x
DMPK	x
DNA-PK				x	x		x
DRAK1	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
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	x		x	x		x
ERK2	x		x	x		x
FAK	x		x		x
FER	x				x
FES/FPS	x				x
FGFR1	x	x			x	x
FGFR2	x	x			x	x	x
FGFR3	x	x			x	x
FGFR4	x	x			x
FGR	x				x
FLT1/VEGFR-1	x	x			x	x
FLT3	x	x			x	x
FLT4	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
IKK alpha	x			x	x
IKK beta	x			x	x
IKK epsilon	x
IR	x	x				x
IRAK1	x
IRAK4	x					x
IRR	x	x
ITK	x
JAK1	x				x
JAK2	x				x
JAK3	x				x	x
JNK1 alpha 1	x				x
JNK2	x				x
JNK3	x				x
KDR/VEGFR-2	x	x			x	x
KHS/MAP4K5
LCK	x				x	x
LKB1 (STK11)	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	x
MARK3	x
MARK4
MEK1	x		x		x
MEK2	x		x		x
MEKK2	x
MEKK3	x
MELK	x
MINK	x					x
MKK6
MLCK/MYLK	x
MLCK2/MYLK2	x
MLK1	x		x
MLK2	x		x
MLK3	x		x
MNK2	x		x
MRCKA/ CDC42BPA	x				x
MRCKB/ CDC42BPB	x				x
MSK1	x
MSK2	x
MSSK1/STK23	x
MST1	x
MST2	x					x
MST3/STK24	x
MST4	x				x
mTOR				x			x
MUSK	x	x			x
NEK1	x				x
NEK2	x
NEK3	x
NEK4	x
NEK6	x
NEK7	x
NEK9	x
NEK11	x
NIK_MAP3K14	x
NLK	x
OSR1	x
P38 alpha	x				x	x
P38 beta	x				x
P38 delta	x				x
P38 gamma	x				x
P70s6k	x		x	x	x
p70s6Kbeta	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
PDGFR alpha	x	x			x	x
PDGFR beta	x	x			x
PDK4							x
PDPK1	x			x
PHK gamma1
PHK gamma2	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
PKC alpha	x		x		x	x
PKC beta1	x		x		x
PKC beta2	x		x
PKC delta	x		x		x
PKC epsilon	x		x		x
PKC eta	x		x		x
PKC gamma	x		x
PKCiota	x		x
PKCmu	x		x
PKCtheta	x		x		x
PKCzeta(PKCz)	x		x
PKD2	x
PKG1 alpha	x
PKG1 beta	x
PKG2/PRKG2	x
PKN1/PRK1	x
PKN2/PRK2	x
PLK1	x				x
PLK2	x					x
PLK3	x
PRKD3/PKCnu	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	x	x			x
ROS	x	x			x
RSK1	x					x
RSK2	x
RSK3	x
RSK4/RPS6KA6	x
SGK1	x				x
SGK2	x
SGK3/SGKL	x
SIK2/SNF1LK2	x
SLK/STK2
SNARK	x
SRMS
STK16
STK22D	x
STK25/YSK1
STK33	x
STK39	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	x	x			x	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
VRK1	x
WEE1	x
WNK2	x
WNK3	x
YES	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)
JAK (V617F)
MNK1(T385D)
p38a(T106M)
PDGFRa(D842V)
PDGFRa(T674I)
PDGFRa(V561D)
RET(V804L)
RET(V804M)

Kinase Profiling & HTS

Kinase Hotspot SM

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

Kinases (Kinase Mutants below)

Kinase Hotspot ^SM