Protein kinases represent one of the most promising groups of drug targets owing to their involvement in such pathological conditions as cancer, inflammatory diseases, neural disorders, and metabolism problems. Read the Expert Opinion review on the challenge of selecting protein assays for lead discovery optimization.
KINASE HOTSPOTSM
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.
Benefits of Kinase HotSpotSM include:
- Gold Standard radiolabeled data: Avoid the false negatives and positives that are generated by fluorescent assay formats;
- 294 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 HotSpotSM 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 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;
- Ki determination;
- Custom Assay development;
- Substrate determination;
- Research collaboration.
RBC can quote any subset of its 294 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 HotSpotSM, 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  |
Download RBC HotSpot Brochure here.
| Tyrosine Receptor 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 (Available soon) |
PKC alpha |
| AKT2 | MLK1 | PKC beta1 |
| AKT3 | MNK2 | PKC beta2 |
| ARAF | P70s6k | PKC delta |
| BRAF | PAK1 | PKC epsilon |
| COT1/MAP3K8 | PAK2 | PKC eta |
| c-SRC | PAK3 | PKC gamma |
| ERK1 | PAK4 | PKC iota |
| ERK2 | PAK5 | PKC mu |
| FAK | PAK6 | PKC theta |
| LYN | PI3Ka (p110a/p85a) | PKCzeta(PKCz) |
| MAPKAPK2 | PI3Kb(p110b/p85a) | PYK2 |
| MAPKAPK3 | PI3Kd (p110d/p85a) | RAF1 |
| MAPKAPK5/PRAK | PI3Kg (p120g) | |
| MEK1 | PKA | |
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| PI3-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 |
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