KinaseProfiler XL
Affordable — High-Quality, Large Scale Kinase Profiling from Millipore, the Upstate Kinase Experts
KinaseProfiler XL analysis reduces the high cost of screening large numbers of compounds. And today, more than ever, controlling cost is an essential step in your drug discovery process. The KinaseProfiler XL service uses a time resolved fluorescence-based high throughput screening platform designed as a cost-effective complement to the industry-first KinaseProfiler service.
The analysis of kinase function is a major focus of drug discovery research today. Current research shows that precise targeting of specific aspects of kinase cascades can provide previously unattainable breakthroughs for therapies of many diseases, including cancer, Alzheimer’s disease and type II diabetes.
The KinaseProfiler XL service offers:
- Rapid turnaround time
- Unprecedented affordability for large scale projects
- Large scale screening of compound libraries against individual kinases (~3,200 data points or more)
- Selectivity profiling against a large kinase panel
- Optional radiometric IC50 analyses on candidates selected in your initial screen
Millipore’s Upstate kinase assay development team continues to be the profiling partner of choice. The KinaseProfiler XL’s HTRF assay enables you to screen your compounds for inhibition of up to 118 kinases, including 84 serine/threonine and 34 tyrosine kinases. At Millipore we offer exceptional diversity, reliability, and affordability for your large-scale kinase profiling projects.
Kinases available on the KinaseProfiler XL analysis panel:
Ser/Thr Kinases (84 Available)*
| ARK (h) | LKB1 (h) | p70S6K (h) | pkg1a (h) |
| ASK1 (h) | LOK (h) | PAK2 (h) | PKG1b (h) |
| Aurora-A (h) | MAPKAP-K2 (h) | PAK3 (h) | Plk3 (h) |
| BrSK1 (h) | MARK1 (h) | PAK4 (h) | PRAK (h) |
| BrSK2 (h) | MELK (h) | PAK6 (h) | PRK2 (h) |
| CaMKlly (h) | MINK (h) | PASK (h) | PrLKX (h) |
| CaMKlV (h) | MLCK (h) | PhKg2 (h) | ROCK-l (h) |
| CHK1 (h) | Mnk2 (h) | Pim-1 (h) | Rsk2 (h) |
| CHK2 (h) | MRCKa (h) | Pim2 (h) | Rsk3 (h) |
| CHK3 (h) | MRCKb (h) | PKA (h) | Rsk4 (h) |
| DAPK1 (h) | MSK1 (h) | PKBγ (h) | SKG (h) |
| DAPK2 (h) | MSK2 (h) | PKCa (h) | SGK2 (h) |
| DCAMKL2 (h) | MSSK1 (h) | PKCσ (h) | SGK3 (h) |
| DMPK (h) | MST1 (h) | PKCε (h) | Snk (h) |
| DRAK1 (h) | MST2 (h) | PKCγ (h) | STK33 (h) |
| DYRK2 (h) | NEK2 (h) | PKCη (h) | TBK1 (h) |
| GRK6 (h) | NEK6 (h) | PKς (h) | TSSK1 (h) |
| HIPK1 (h) | NEK11 (h) | PKCμ (h) | TSSK2 (h) |
| HIPK2 (h) | NEK3 (h) | PKCθ (h) | WNK2 (h) |
| HIPK3 (h) | NEK7 (h) | PKOξ (h) | WNK3 (h) |
| IKKβ (h) | NLK (h) | PKD2 (h) | ZIPK (h) |
Tyrosine Kinases (34 Available)*
| Bmx | EphA2 | IR |
| c-Kit (D816H) | ErbB4 | JAK2 |
| c-Kit | FAK | JAK3 |
| c-Kit (D816V) | FGFR1 | Lck |
| c-Kit (V560G) | FBFR2 | Lyn |
| CSK | FGFR2 (N549H) | MER |
| cSrc | FGFR4 | Met |
| EGFR | Fgr | Ron |
| EGFR (L861Q) | Flt3 | TrkB |
| EGFR (L858R) | Flt3 (D835Y) | ZAP-70 |
| EGFR (T790M) | Flt4 | |
| EGFR (T790M, L858R) | Hck |
KinaseProfiler XL Services make it easy for you to conduct detailed follow-up analyses. Utilizing best-in-class Upstate kinases developed by our team of kinase experts, Millipore’s KinaseProfiler XL service is the only choice for your large-scale kinase screening needs. Our service enables you to investigate the inhibition profiles of many drug candidates against a focused kinase panel, or perform early safety and selectivity screens of a few critical inhibitors against a broad array of kinases. You can also specify criteria for automatic KinaseProfiler IC50 analyses on any number of inhibitors from your primary screen without the need for re-ordering, or duplicate compound submission.
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KinaseProfiler XL’s HTRF® Assay
The KinaseProfiler XL service offers you the flexibility to affordably design your own high-content profile without sacrificing quality or data integrity.
Cost-effective large scale kinase profiling with KinaseProfiler XL analysis enables you to see a variety of new patterns and trends among your drug candidates to help you better understand structure activity relationships and mechanisms of action.
KinaseProfiler XL Assay Specifications:
Minimum 3,200 wells per kinase (10 plates)
Reference inhibitors available (additional charges may apply)
Data will be provided as an Excel file showing % control activity
Compound Requirements:
Compounds to be provided as 50X stock in 100% DMSO
30 μL minimum per well (single kinase)
200 μL minimum per well (full panel)
Compounds to be delivered pre-plated in 384 well plates according to Millipore plate plan
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