ROCK1 Human AGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW
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:
Fragment (17-535), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant protein kinase ROCK1 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.13 U/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 15 μM long S6 kinase substrate, 10 μM ATP and 0.25 μCi [γ32P]ATP for another 30 minutes incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Long S6 kinase substrate formed. Compounds are screened at 10 μM.
Substrate:
15 µM Long S6 kinase substrate peptide
ATP Concentration:
10 uM
Incubation:
30 min at 37°C
Control Inhibitor:
Rho-Kinase inhibitor
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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