Cart
sales@molnova.com
GSK429286A
CAS No. 864082-47-3
GSK429286A( GSK429286A | GSK 429286A )
Catalog No. M17626 CAS No. 864082-47-3
GSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 60 | In Stock |
|
| 2MG | 33 | In Stock |
|
| 5MG | 53 | In Stock |
|
| 10MG | 81 | In Stock |
|
| 25MG | 132 | In Stock |
|
| 50MG | 200 | In Stock |
|
| 100MG | 343 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameGSK429286A
-
NoteResearch use only, not for human use.
-
Brief DescriptionGSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
-
DescriptionGSK429286A 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.
-
In VitroGSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM.
-
In VivoGSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg.
-
SynonymsGSK429286A | GSK 429286A
-
PathwayOthers
-
TargetOther Targets
-
RecptorROCK1| ROCK2
-
Research AreaCancer
-
Indication——
Chemical Information
-
CAS Number864082-47-3
-
Formula Weight432.37
-
Molecular FormulaC21H16F4N4O2
-
Purity>98% (HPLC)
-
SolubilityDMSO : ≥ 51 mg/mL; 117.95 mM
-
SMILESCC1=C(C(CC(=O)N1)c1ccc(cc1)C(F)(F)F)C(=O)Nc1c(cc2c(c1)cn[nH]2)F
-
Chemical NameN-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Goodman KB, et al. J Med Chem, 2007, 50(1), 6-9.
molnova catalog
related products
-
(9,10-DiHOME
±)9,10-DiHOME is the racemate of 9,10-DiHOME. 9,10-DiHOME is a leukotoxin derivative of linoleic acid diol that has been reported to be toxic in human's tissue preparations, and is produced by inflammatory leukocytes such as neutrophils and macrophages.
-
NPAS3-IN-1
NPAS3-IN-1 is a potent inhibitor of NPAS3-ARNT heterodimerization, modulating NPAS3 transcription by targeting the interaction between NPAS3 and ARNT at the cellular level.
-
Tubulin polymerizati...
Tubulin polymerization-IN-47 is a tubulin polymerization inhibitor and mitotic inhibitor with antitumor activity and inhibitory effects on neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell lines, respectively.
