OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
LIM domain kinases 1 and 2 (LIMK1 and LIMK2) play a critical role in stimulus-induced remodeling of the actin cytoskeleton by linking signals from the Rho family GTPases. LIMKs specifically phosphorylate and inactivate cofilin, an actin-binding protein that stimulates depolymerization and severance of actin filaments, thereby regulating actin cytoskeletal reorganization. Inhibition of LIMK1 may be useful in the treatment of tumors, especially invasive breast and prostate cancer cells.
Family:
Kinase
Sub Family:
TKL
Class:
Protein Ser/Thr
Protein Name:
LIMK1
Uniprot Number:
P53667
Protein Aliases:
LIM domain kinase 1|LIMK-1
Gene Name:
LIMK1
Gene ID:
3984
Gene Aliases:
LIMK
Accession Number:
NM_002314
Organism:
Human
Construct Details:
285-638 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
LIMK1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.6 mg/mL cofilin, 10 mM MgAcetate and [gamma-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:
0.6 mg/mL cofilin
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 22.22µM )
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:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibition of LIMK1 may be useful in the treatment of tumors, especially invasive breast and prostate cancer cells.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
LIMK1 Human TKL Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-656KP
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