864082-47-3 Usage
Uses
GSK 429286 is a selective Rho-kinase (ROCK) inhibitor.It is orally available and has been shown to dramatically reduce mean arterial pressure in spontaneously hypertensive rats.
Biological Activity
gsk429286a is a selective inhibitor of rock1 and rock2 with ic50 value of 14 nm and 63 nm, respectively [1].rho-kinase (rock) is a member of agc (protein kinase a, protein kinase g and protein kinase c) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].gsk429286a is a potent rock inhibitor and has a different activity with the reported rock inhibitor y27632. using gst method, it is shown that gsk429286a treatment (10 μm) increased mypt phosphrylation at thr850 via inhibiting rock which mediated this phosphorylation process [3].in male sprague-dawley rat model with spontaneously hypertensive, oral administration of gsk429286a (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmhg after nearly 2 h treatment [4].
references
[1]. nichols, r.j., et al., substrate specificity and inhibitors of lrrk2, a protein kinase mutated in parkinson's disease. biochem j, 2009. 424(1): p. 47-60.[2]. shi, j., et al., distinct roles for rock1 and rock2 in the regulation of cell detachment. cell death dis, 2013. 4: p. e483.[3]. davis, d.a., et al., increased therapeutic potential of an experimental anti-mitotic inhibitor sb715992 by genistein in pc-3 human prostate cancer cell line. bmc cancer, 2006. 6: p. 22. [4]. goodman, k.b., et al., development of dihydropyridone indazole amides as selective rho-kinase inhibitors. j med chem, 2007. 50(1): p. 6-9.
Check Digit Verification of cas no
The CAS Registry Mumber 864082-47-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,4,0,8 and 2 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 864082-47:
(8*8)+(7*6)+(6*4)+(5*0)+(4*8)+(3*2)+(2*4)+(1*7)=183
183 % 10 = 3
So 864082-47-3 is a valid CAS Registry Number.
864082-47-3Relevant articles and documents
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors
Goodman, Krista B.,Cui, Haifeng,Dowdell, Sarah E.,Gaitanopoulos, Dimitri E.,Ivy, Robert L.,Sehon, Clark A.,Stavenger, Robert A.,Wang, Gren Z.,Viet, Andrew Q.,Xu, Weiwei,Ye, Guosen,Semus, Simon F.,Evans, Christopher,Fries, Harvey E.,Jolivette, Larry J.,Kirkpatrick, Robert B.,Dul, Edward,Khandekar, Sanjay S.,Yi, Tracey,Jung, David K.,Wright, Lois L.,Smith, Gary K.,Behm, David J.,Bentley, Ross,Doe, Christopher P.,Hu, Erding,Lee, Dennis
, p. 6 - 9 (2007/10/03)
Rho kinase (ROCK1) mediates vascular smooth muscle contraction and is a potential target for the treatment of hypertension and related disorders. Indazole amide 3 was identified as a potent and selective ROCK1 inhibitor but possessed poor oral bioavailabi
