Cofttek holdings limited

TGF-beta&Smad

GSK429286A (864082-47-3)

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. GSK429286A is a selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively).

Not Intended for Therapeutic Use. For research use only.

CAS: 864082-47-3 Category

GSK429286A (864082-47-3) Description:

GSK429286A is a selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.

ROCK inhibitors have been found to prevent apoptosis, as well as enhance the survival and cloning efficiency of dissociated human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency.

GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK).

It less potently inhibits p90 and p70 ribosomal S6 kinases (IC50s = 780 and 1,940 nM, respectively) and is ineffective against leucine-rich repeat protein kinase-2. GSK429286A reverses adrenalin-induced contraction of rat aortic rings (IC50 = 190 nM) and produces a dose-dependent decrease in mean arterial pressure in spontaneously-hypertensive rats.

GSK429286A (864082-47-3) Specifications:

Product Name GSK429286A
Synonyms GSK 429286A; GSK-429286A;RHO-15
Chemical Name ~{N}-(6-fluoro-1~{H}-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1~{H}-pyridine-5-carboxamide
Purity >98%
CAS Number 864082-47-3
Molecular Formula C21H16F4N4O2
Molecular Weight 432.379 g/mol
Monoisotopic Mass 432.121 g/mol
MDL number MFCD16618404
InChIKey OLIIUAHHAZEXEX-UHFFFAOYSA-N
InChi Code InChI=1S/C21H16F4N4O2/c1-10-19(20(31)28-17-6-12-9-26-29-16(12)8-15(17)22)14(7-18(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-6,8-9,14H,7H2,1H3,(H,26,29)(H,27,30)(H,28,31)
SMILES CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F
Form powder
Color white
Solubility  Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application Selective Rho-kinase (ROCK) inhibitor; ROCK Inhibitor

 


=

RIDADR NONH for all modes of transport

References:

  • Extracellular heat shock protein 90α mediates HDM-induced bronchial epithelial barrier dysfunction by activating RhoA/MLC signaling. Dong HM, Le YQ, Wang YH, Zhao HJ, Huang CW, Hu YH, Luo LS, Wan X, Wei YL, Chu ZQ, Li W, Cai SX. Respir Res. 2017 May 30;18(1):111. doi: 10.1186/s12931-017-0593-y.
  • ROCK inhibition abolishes the establishment of the aquiferous system in Ephydatia muelleri (Porifera, Demospongiae). Schenkelaars Q, Quintero O, Hall C, Fierro-Constain L, Renard E, Borchiellini C, Hill AL. Dev Biol. 2016 Apr 15;412(2):298-310. doi: 10.1016/j.ydbio.2016.02.026. Epub 2016 Mar 2.
  • Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson’s disease. Nichols RJ, Dzamko N, Hutti JE, Cantley LC, Deak M, Moran J, Bamborough P, Reith AD, Alessi DR. Biochem J. 2009 Oct 23;424(1):47-60. doi: 10.1042/BJ20091035.

1 review for GSK429286A (864082-47-3)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The GSK429286A (864082-47-3) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *