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:
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Gold Standard radiolabeled data: Avoid the false negatives and positives that are generated by fluorescent assay formats;
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341 kinase assays available, and growing;
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Costs can be as low as outsourced fluorescent screens;
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HotSpot's low cost lets you profile more compounds earlier, and avoid dead-end leads;
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HotSpot HTS brings economic radiolabeled assaying to HTS: Shorten your hit validation timeline;
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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:
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Larger scale HTS;
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Large scale single dose, duplicate profiling;
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IC50 profiling — 5 or 10 dose with curve fitting;
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ATP — competitive evaluation;
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Compound binding reversibility test;
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Ki determination;
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Custom Assay development;
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Substrate determination;
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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/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 | |
| 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 |
 |
||
| 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 | |
 |
||
| 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 |
| 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 | |
KINOME MAPPING APP. DISPLAY YOUR SCREENING RESULTS WITH RBC'S FREE APPLICATION HERE
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)
