OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Rho-associated, coiled-coil containing protein kinase (ROCK), including the ROCK1 and ROCK2 isoforms, is a protein kinase involved in signaling from Rho to actin cytoskeleton. PKA and the two ROCKs have been reported to have opposite effects on neurite formation. More studies are needed to provide significant insights into the role of ROCK in several pathological processes. ROCK inhibitors have been shown the benefit for treatment of various cancers, inflammation, coronary artery spasms and hypertension.
Family:
Kinase
Sub Family:
AGC
Class:
Protein Ser/Thr
Protein Name:
ROCK1
Uniprot Number:
Q13464
Protein Aliases:
Renal carcinoma antigen NY-REN-35|Rho-associated, coiled-coil-containing protein kinase 1|Rho-associated, coiled-coil-containing protein kinase I|ROCK-I|p160 ROCK-1|p160ROCK
Gene Name:
ROCK1
Gene ID:
6093
Gene Aliases:
p160ROCK
Accession Number:
NM_005406
Organism:
Human
Construct Details:
17-535 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
ROCK-I (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 µM KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK, 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:
30 uM KEAKEKRQEQIAKR
Tracer:
33P
ATP Concentration:
[ATP]= 70µM (Km= 73µM )
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
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
ROCK1 Human AGC Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-601KP10
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