Kinase Profiling & HTS
Kinase Hotspot SM
Pharma labs typically only use P33 radiolabeled profiling for only a few select compounds. Now, RBC's proprietary nanoliter screening techniques make this gold standard 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 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;
- 325 kinases 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:
Assay Type |
Sample Price* |
| HTS — 1 kinase | $3.00 / well: 20,000 compound order |
| 10 dose IC50 vs 50 kinase panel |
$50 / IC50: 20 compounds |
| 10 dose IC50 vs 100 kinase panel |
$40 / IC50: 20 compounds |
| 10 dose IC50 vs 200 kinase panel |
$30 / IC50: 20 compounds |
* The price is subject to change and discounts may apply for larger orders. Please call 1-877-347-2368 for details.
Kinase 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 325 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 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 | COT1/MAP3K8 | mTOR |
| AKT2 | DNA-PK | P70s6k |
| AKT3 | ERK1 | PDPK1 |
| ARAF | ERK2 | PI3Ka (p110a/p85a) |
| ASK1 | GSK3a | PI3Ka (p110b/p85a) |
| BRAF | GSK3B | PI3Ka (p110d/p85a) |
| CHK1 | IKK alpha | PI3Kg (p120g) |
| CHK2 | IKK beta | RAF1 |
 |
||
| 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 alpha2 | 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) | DNA-PK | PI3Ka (p110a/p85a) |
| AMPK(A1/B1/G2) | EIF2AK2 | PI3Kb (p110b/p85a) |
| AMPK(A1/B2/G1) | FGFR2 | PI3Kd (p110d/p85a) |
| AMPK(A2/B1/G1) | mTOR | PI3Kg(p120g) |
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)
