Kinase Screening and Profiling Services

Accelerate your drug discovery program with Kinase Screening and Profiling Services from BPS Bioscience, Inc. Trust us to provide you with high quality data with fast turnaround time. Our team of experts along with our broad services portfolio makes it easy to:

  • Screen for inhibitors/targets using our unique panel of 20+ assays
  • Select from IC50 determination and single point concentrations
  • Receive data within days of compound submission
  • Perform follow-up studies using the same proteins manufactured in-house
  • Get questions answered or project guidance in a time-efficient manner

Biochemical Assays:

Abl CDK9/CyclinT1 FGFR2 PLK1
Abl-1 (T315I) CK1 Flt1 RET
Abl-1 (T315I) cKit Flt1 RET
AKT cMet FYN ROS1
ALK cRAF GSK3a PI3Kα (p110α/p85α)
Aurora A CSF1R GSK3b PI3Kβ (p110β/p85α)
BRAF c-Src HER2 PI3Kδ (p110δ/p85α)
BRAF (V600E) EGFR (WT) HER4 PI3Kγ (p110γ/PIK3R5)
BTK EGFR (L858R) IKKβ SYK
CDK1/CyclinB1 EGFR (T790M) Jak2 TAK1-TAB1
CDK2/CyclinA2 EGFR (L858R, T790M) Jak3 TRKA
CDK4/CyclinD3 EGFR (T790M, C797S,
L858R) 
Lck TRKB
CDK5/p25 EGFR (murine) MNK1 (T385D) TYK2
CDK6/CyclinD3 EphA2 p38 VEGFR2/KDR
 CDK7/CyclinH1/MNAT1 FAK    

Background:

Protein phosphorylation is a key aspect in the regulation of a large number of cellular processes including cellular division, metabolism, signal transduction, and many more. There are over 500 kinases encoded by the human genome and it has been estimated that kinases regulate approximately 50% of cellular functions. Kinase is the name given to an enzyme that catalyzes the transfer of a phosphate group from ATP to another molecule. Kinases can be broadly separated by their substrate into protein and lipid kinases with the protein kinases being further classified based on their cellular location and the specific amino acid(s) they phosphorylate; cytoplasmic threoninereceptor tyrosine kinases (RTKs), and serine/threonine.

The prominent roles that kinases play in cell division have made them attractive targets for both immunosuppressant drugs and cancer therapeutics. Kinases are highly druggable, and account for over 25% of targets screened by the pharmaceutical industry. Currently, there are over 25 kinase inhibitors that have been approved for clinical use by the FDA, including rapamycin, which was discovered in the 1960s. It was not until three decades later, however, that the target of rapamycin was discovered to be a serine/threonine kinase that was named mammalian target of rapamycin (mTOR). Today rapamycin is approved as an immunosuppressant and a number of mTOR inhibitors are being investigated as treatments for various forms of cancer.

BPS offers a wide selection of kinaseskinase substrates and kinase inhibitors. Our kinases are validated through rigorous QC testing and are suitable for use in nearly all in vitro kinase assays. We also offer kinase inhibitor screening services.

References:

1.   Cohen, P. Nat. Rev. Drug Disc. 2002; 1: 309-315. 
2.   Ballou, L.M., et al., J. Chem. Biol. 2008 1(1-4): 27-36.
3.   Loewith, R., et al., Genetics. 2011; 189(4): 1177-1201.