OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
the never-in-mitosis kinase (NEK) family is emerging as novel kinase targets in various cancer types. NEK5 is an understudied member of the NEK family. While there are more recent studies describing the physiologic function of NEK5, its role in cancer biology remains widely understudied. However, emerging studies implicate that NEK5 has potentially crucial functions in various solid tumors. In this review, we discuss current knowledge regarding the role of NEK5 in cancer and the implications of NEK5 expression and activity in tumor development and metastasis. We summarize current studies that examine NEK5 activity in diverse cancer systems and cellular processes. As an understudied kinase, there are currently no selective NEK5-targeting agents to test the effects of pharmacologic inhibition on cancer, although there exist recent advancements in this area. Here we also include an update on efforts to develop selective pharmacologic inhibition of NEK5, and we discuss the current direction of NEK5-targeting therapeutic development. The generation of selective NEK5 inhibitors is promising new targeted therapies for cancer growth and metastasis.
Family:
Kinase
Sub Family:
CAMK
Class:
Protein Serine/Threonine
Protein Name:
NEK5
Uniprot Number:
Q6P3R8
Protein Aliases:
Serine/threonine-protein kinase Nek5|Never in mitosis A-related kinase 5 (NimA-related protein kinase 5)
Gene Name:
NEK5
Gene ID:
341676
Gene Aliases:
NA
Organism:
Human
Construct Details:
1-311
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
NEK5 (h) is incubated with 20 mM Tris/HCl pH 8.5, 0.2 mM EDTA, 250 µM RLGRDKYKTLRQIRQ, 10 mM Magnesium acetate and [?-33P-ATP] (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting
Substrate:
250 µM RLGRDKYKTLRQIRQ
Tracer:
33P
ATP Concentration:
[ATP]= 200µM (Km= 305.6µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Staurosporine
Test Sample Requirements:
Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cancer/Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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