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Application: Study enzyme kinetics and screen small molecular inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: ROCK2 (Rho-associated coiled-coil protein kinase 2), an isoform of ROCK1, is a serine/threonine kinase target of small GTPase Rho that regulates the formation of actin stress fibers and focal adhesions, cytokinesis, and smooth muscle contraction. It is therefore important for proper vascular function and is involved in a number of fibrotic pathologies. The ROCK2 inhibitor Fasudil has been investigated for the treatment of cerebral cavernous malformation (CCM), which causes brain hemorrhages, and is in clinical trials for other applications such as Amyotrophic Lateral Sclerosis (ALS). Belumosudil, a newer ROCK2 inhibitor, was approved by the FDA for chronic graft versus host disease in 2021. The development of new inhibitors will continue to bring new treatments options to patients with ROCK2 related disorders.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ ROCK2 Kinase Assay Kit is designed to measure ROCK2 (Rho-associated coiled-coil protein kinase 2) serine/threonine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The ROCK2 Kinase Assay Kit comes in a convenient 96-well format, with enough purified ROCK2 (amino acids 5-554), substrate, ATP, and kinase assay buffer for 100 enzyme reactions.Need us to run inhibitor screens or profile your compounds against ROCK2 ? Check out our Kinase Screening Services.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Target: ROCK2
Uniprot: O75116
Unit Definition: Assay Kit
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: Lochhead P. A., et al., 2010 Oncogene 29.17: 2591-2598.Zheng Biqiang, et al., 2011 Clinical Cancer Research 17.24: 7574-7583.
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