1072906-02-5 Usage
Description
Rho Kinase Inhibitor V, also known as a pyrazolyl carboxamide compound, is a cell-permeable molecule that serves as a potent inhibitor of ROCK-II with an IC50 of 1.5 nM. It effectively inhibits the myosin light chain 2 phosphorylation on Thr18/Ser19 in A7r5 cells, with an IC50 of 72 nM. Additionally, it impacts the activities of PKA, MRCK, Akt1, and CYP-450 enzymes, but only at significantly higher concentrations.
Uses
Used in Pharmaceutical Industry:
Rho Kinase Inhibitor V is used as a research compound for studying the role of ROCK-II in various cellular processes and diseases. Its application is crucial in understanding the underlying mechanisms of ROCK-II inhibition and its potential therapeutic benefits.
Used in Cell Biology Research:
Rho Kinase Inhibitor V is used as a tool in cell biology research to investigate the effects of ROCK-II inhibition on cell signaling pathways, cell migration, and cell proliferation. This helps researchers gain insights into the potential applications of ROCK-II inhibition in the treatment of various diseases.
Used in Drug Development:
Rho Kinase Inhibitor V is used as a lead compound in the development of new drugs targeting ROCK-II for the treatment of diseases where ROCK-II plays a significant role, such as cardiovascular diseases, neurological disorders, and cancer.
Used in Biochemical Assays:
Rho Kinase Inhibitor V is used as a specific inhibitor in biochemical assays to assess the activity of ROCK-II and its contribution to various cellular processes. This helps in determining the effectiveness of the inhibitor and its potential as a therapeutic agent.
Check Digit Verification of cas no
The CAS Registry Mumber 1072906-02-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,7,2,9,0 and 6 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1072906-02:
(9*1)+(8*0)+(7*7)+(6*2)+(5*9)+(4*0)+(3*6)+(2*0)+(1*2)=135
135 % 10 = 5
So 1072906-02-5 is a valid CAS Registry Number.
1072906-02-5Relevant articles and documents
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors
Feng, Yangbo,Yin, Yan,Weiser, Amiee,Griffin, Evelyn,Cameron, Michael D.,Lin, Li,Ruiz, Claudia,Schürer, Stephan C.,Inoue, Toshihiro,Rao, P. Vasanth,Schr?ter, Thomas,LoGrasso, Philip
supporting information; experimental part, p. 6642 - 6645 (2009/10/23)
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ～3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.
