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Rho-associated Protein Kinase (ROCK) Inhibitors

April 9, 2018

Rho-associated protein kinase (ROCK) belongs to the family of serine/threonine kinases. Research shows that ROCK signaling plays a role in several diseases, including diabetes, Parkinson’s, amyotrophic lateral sclerosis, pulmonary hypertension, and cancer.

A new study published in January 2017 demonstrates that ROCK2 has a larger impact on the regulation of Ewing sarcoma (EWS) malignancy than ROCK1. In patient-derived cell lines, ROCK2 expression was higher in the metastasis derived cell line compared to the primary tumor derived cell line. Gaining a better understanding of ROCK inhibition may provide new insights on treatment of sarcomas1.

Another study found that inhibition of the RhoA/ROCK pathway has a protective effect on glomerular inflammation found in diabetic nephropathy. Treatment with the inhibitor Y27632 decreased the release of adhesion molecules in rat glomerular endothelial cells incubated with advanced glycation end products. Blocking this pathway protects the kidneys and improves kidney function without causing inflammation2.

 

LKT Labs offers several high purity ROCK inhibitors for research use.

F0275 Fasudil Hydrochloride

G7443 GSK-429286A  

H0003 H89

P0255 Pantoprazole

P0256 Pantoprazole Sodium Sesquihydrate

R4132 RKI-1447 

T3132 Thiazovivin

V9201 VX-11e

Y1000 Y27632 Dihydrochloride

 

1. Oncol Rep. 2017 Jan 20. doi: 10.3892/or.2017.5397. Targeting ROCK2 rather than Rock1 inhibits Ewing sarcoma malignancy. [Epub ahead of print]

2. Sci Rep. 2017 Jan 5;7:39727. doi: 10.1038/srep39727. Inhibition of the RhoA/ROCK pathway can benefit the kidneys in diabetics.

Categories: News

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