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Kinase Inhibitor Screening Service
BioAssay Systems has developed and validated a variety of proprietory methods for follow-up study and HTS screening of kinase inhibitors.
1. IMAP Kinase Assay
This fluorescence polarization assay is based on the specific binding of the kinase reaction product, a fluorescent labeled phosphopeptide, to metal-nanoparticles, thus slowing down the rotation of the peptide in solution.
Typical assay optimization steps include enzyme (Figure A) and substrate titrations, interference by dimethyl sulfoxide (DMSO) and Z’ factor determination. For screening kinase inhibitors, the inhibitor is usually incubated with the kinase for 10 min prior to addition of ATP and substrate. Z’ factors of >0.8 are often observed in these assays.
Please contact us by email or call 1-510-782-9988 x 2 to discuss your kinase screening service needs.
Please contact us by email or call 1-510-782-9988 x 2 to discuss your kinase screening service needs.
2. EKIN Kinase Assay
Our proprietary, homogeneous, microplate-based EKIN kinase assay involves incubating the kinase with a single working reagent. During the kinase reaction, ATP is converted to ADP. The produced ADP is enzymatically converted to ATP and pyruvate, which is quantified using a fluorimetric (530nm/590nm) assay method.
Please contact us by email or call 1-510-782-9988 x 2 to discuss your kinase screening service needs.
Publications
Rommel Mallaria, Elissa Swearingenb, Wei Liu, Arnold Ow, Stephen W. Young and Shu-Gui Huang* (2003) “A Generic High- throughput Screening Assay for Kinases: Protein Kinase A as an Example”. J. Biomol. Screen. 8: 198-204.
Catherine A. Hong, Elissa Swearingen, Rommel Mallari, Xiong Gao, Zhaodan Cao, Anne North, Stephen W. Young and Shu-Gui Huang* (2003) “Development of A High-Throughput Time-Resolved Fluorescence Resonance Energy Transfer Assay for TRAF6 Ubiquitin Polymerization”. Assay and Drug Development Technologies 1: 175-180.
Shu-Gui Huang* (2002) “Development of A High-throughput Screening Assay for Mitochondrial Membrane Potential in Living Cells”. J. Biomol. Screen. 7: 383-389.
Ellyn Farrelly, M. Catherine Amaral, Lisa Marshall and Shu-Gui Huang* (2001) A high-throughput assay for mitochondrial membrane potential in permeabilized yeast cells. Analytical Biochemistry 293(2):269-276.
Tony Smith, John Chan, Donna Oksenberg, Roman Urfer, Dave Wexler, Arnie Ow, Liping Gao, Alanna McAlorum, and Shu-Gui Huang* (2004). A High-Throughput Turbidometric Assay for Screening Inhibitors of Protein Disulfide Isomerase Activity. J. Biomol. Screen. 9(7): 614-620.
David S. Wexler, Liping Gao, Francisco Anderson, Arnold Ow, Laszlo Nadasdi, Alanna McAlorum, Roman Urfer, and Shu-Gui Huang* (2005). “Linking Solubility and Permeability Assays for Maximum Throughput and Reproducibility”. J. Biomol. Screen. 10(4): 383-390.
Shu-Gui Huang (2005) “Progress from HTS to HTL: Current Strategies in Drug Lead Discovery” Review article in Trends in Pharmaceutical Research 1: 5-10.
David S. Wexler, Shu-Gui Huang, Roman Urfer (2004). “Replumbing the Pipeline: A small, biopharmaceutical company’s strategy for integrating lead optimization and ADMET screening”. Current Drug Discovery, May 2004: 35-38.
Shu-Gui Huang, Donna Oksenberg, Roman Urfer (2005). “High-throughput Turbidometric Assay for Screening Inhibitors of Protein Disulfide Isomerase Activity”. US 6,977,142.
Customer Testimonials
"The guys at BioAssay Systems know their science! I had to develop a bioassay for our company and Robert was very quick to respond to keep us up to date. They are knowledgeable and very resourceful. They directed us to one of the bulk suppliers that could give us a really good deal on our active ingredient. They keep very detailed records for our research needs. I would recommend working with BioAssay Systems on your assay development projects!"
"It is a pleasure working together with BioAssay Systems. I brought samples to their Hayward location and received the results in less than 24 hr. The discussion with Robert Z was courteous, open, and with a depth of knowledge. Robert has a PhD from Stanford. Also, Frank Huang, the CEO, had sufficient scientific curiosity to try out our cleanser and provide feedback! This is beyond the call of customer relations. BioAssay Systems is a company with a lot of expertise and a friendly, responsive approach to problem solving. I will enthusiastically continue to work with them to carry out our research."
"I would like to show my appreciation to the Bioassay Systems service team. We are developing an assay to measure the change in lactate concentration of single cell samples using fluorescent microscopy. The BioAssay Systems team was quite helpful in assisting us to optimize their fluorescent L-Lactate assay kit for our unique experimental set-up. The BioAssay Systems team is always friendly and knowledgeable. We know that we can rely on them for fast and professional service."
"While developing biodegradable coatings for Drug Eluting Stents I worked with Bob to develop an accurate, precise and sensitive assay for determining the amount of polymer remaining in tissue. It was a pleasure to work with Bob and his team, they are very thorough, they understand the science very well and they always deliver on time and at the right price. I would highly recommend anyone using BioAssay Systems services in the future."
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