Product Description
Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.
IC50 & Target: Ki: 220/300 nM (ROCK-I/II)[1]
In Vitro: Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively[1]. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 µM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 µM Y-27632 induced group[2].
In Vivo: Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group[3]. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group)[4].
Information
CAS No146986-50-7
FormulaC14H21N3O
Clinical Informationclinicalinformation
PathwayApoptosis
Cell Cycle/DNA Damage
Cytoskeleton
Stem Cell/Wnt
TGF-beta/Smad
TargetApoptosis
ROCK
Specifications
FormWhite to off-white (Solid)
Purity / Grade99.89%
SolubilityDMSO : 50 mg/mL (202.15 mM; Need ultrasonic);
H2O : 1 mg/mL (4.04 mM; ultrasonic and warming and heat to 60°C)
SmilesO=C([C@@H]1CC[C@]([C@H](N)C)([H])CC1)NC2=CC=NC=C2
Misc Information
Storage Instruction-20°C, protect from light, stored under nitrogen
Alternative NamesCyclohexanecarboxamide, 4-[(1R)-1-aminoethyl]-N-4-pyridinyl-, trans
Observed Molecular Weight247.34
References[1]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
[2]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem
cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5.
[3]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.
[4]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.
[5]. Maldonado M, et al. ROCK inhibitor primes human induced pluripotent stem cells to selectively differentiate towardsmesendodermal lineage via
epithelial-mesenchymal transition-like modulation. Stem Cell Res. 2016 Sep;17(2):222-227.
[6]. Kan L, et al. Rho-Associated Kinase Inhibitor (Y-27632) Attenuates Doxorubicin-Induced Apoptosis of Human Cardiac Stem Cells. PLoS One.
2015;10(12):e0144513. Published 2015 Dec 8.
[7]. Zhang L, et al. ROCK inhibitor Y-27632 suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells and increases their cloning
efficiency. PLoS One. 2011;6(3):e18271. Published 2011 Mar 28.
[8]. Svoboda KK, et al. ROCK inhibitor (Y27632) increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium. Dev Dyn.
2004;229(3):579-590.