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ROCK inhibitor Y-27632

(HB2297)
Data

Product overview

  • Name
    ROCK inhibitor Y-27632
  • Short description
    Y-27632 is a selective ROCK inhibitor
  • Biological description

    The ROCK inhibitor Y-27632 is a selective and cell permeable inhibitor of the Rho-associated protein kinase (ROCK) (Ki values are 0.14, 26 ,25 and >250 µM at p160ROCK, PKC, PKA and MLCK respectively).


    Y-27632 has many biological actions and is an important small molecule modulator of stem cells. It diminishes hES and hiPSC dissociation-induced apoptosis, enhances survival and colony formation of dissociated hESC without affecting pluripotency or self-renewal.


    Y-27632 also improves hESC and iPSCs postthaw viability and survival rate during cryopreservation.


    Additionally, Y-27632 inhibits smooth muscle contractility and shows antihypertensive effect. 

  • Alternative names
    Y27632 dihydrochloride
  • Biological action
    Inhibitor
  • Purity
    >99%
  • Customer comments

    The ROCK inhibitor Y-27632 is working as expected. Verified customer, University of Louisville

  • Citations

Images

Properties

  • Chemical name
    trans-4-[(1R)-1-Aminoethyl]-N-4-pyridinylcyclohexanecarboxamide dihydrochloride
  • Molecular Weight
    320.26
  • Chemical structure
    Y-27632 dihydrochloride [129830-38-2]
  • Molecular Formula
    C14H21N3O.2HCl
  • CAS Number
    129830-38-2
  • PubChem identifier
    9901617
  • SMILES
    C[C@H](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl
  • Source
    Synthetic
  • InChi
    InChI=1S/C14H21N3O.2ClH/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13;;/h6-12H,2-5,15H2,1H3,(H,16,17,18);2*1H/t10-,11?,12?;;/m1../s1
  • InChiKey
    IDDDVXIUIXWAGJ-DDSAHXNVSA-N
  • MDL number
    MFCD03490488
  • Appearance
    White solid

Applications

  • Application notes

    Introduction

    Rho kinase (Rho-associated coiled coil protein kinase or ROCK) is a major downstream effector for the small GTP-binding protein Rho [1]. Rho kinase is involved in various biological processes including cell mitosis adhesion, cytoskeletal adjustments, muscle cell contraction, tumor cell invasion and a series of cell biological phenomena [2]. Through a series of cascading effects, Rho kinase influences actin and microtubule regulation of apoptosis and thus plays a key role in early embryonic development [3].The Rho kinase signalling pathway is highly activated in many pathological conditions [4].

    Rock inhibitor Y-27632 is a Rho kinase inhibitor which selectively inhibits p160ROCK (ROCK1) with a Ki value of 140 nM and binds to the Rho kinase ATP binding pocket in an ATP-competitive manner [5].


    Uses

    Y-27632 has been shown to have a diverse range of actions and has been used in a variety of biological systems. It is the most commonly used of the ROCK inhibitors in stem cell research and is used as a multifunctional reagent in many stem cell related processes [6]. Y-27632 demonstrates many positive effects across various cell types, in particular human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs) [7] and has greatly improved a number of practical stem cell procedures [8]. For example it has been shown that Y-27632 increases cell adhesion and proliferation and increases post-thaw cell survival and post-passaging cell viability [9,10].


    Cellular dissociation

    Cell dissociation is one of the most common manipulations in stem cell research. During cellular dissociation both hESC and hIPSCs are vulnerable to dissociation-induced apoptosis or anoikis (a form of apoptosis induced by inappropriate cell-cell or cell-ECM interactions) [3,11]. Y-27632 is of particular interest as it allows hPSCs to escape this dissociation-induced apoptosis. Y-27632 prevents apoptosis of dissociated hPSCs and increases their survival rate and plating efficiency [11].


    Cryopreservation

    Cryopreservation is also an important part of stem cell research. Y-27632 improves the recovery of cryopreserved hPSCs and has greatly helped simplify the cryopreservation procedure. The slow-freezing and rapid-thawing procedure which uses DMSO as a cryoprotectant is commonly used in stem cell cryopreservation, however this method is not suitable for hPSCs, therefore vitrification (fast freezing, slow thawing) is used [12]. Vitrified hPSCs do however still suffer from high levels of cell death and do not passage well as single cells [11]. The addition of Y-27632 to freezing and post-thawing medium enhances colony formation efficiency and treatment with Y-27632 during cryopreservation also increases survival rate and cell adhesion of freeze-thawed dissociated hES [12].

Storing and Using Your Product

  • Storage instructions
    Room temperature (desiccate)
  • Solubility overview
    Soluble in water (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for ROCK inhibitor Y-27632

  • 1, Rho-kinase/ROCK: A key regulator of the cytoskeleton and cell polarity.

    Amano et al (2010) Cytoskeleton (Hoboken) 67(9) : 545-54
    PubMedID: 20803696
  • 2, Rocks: multifunctional kinases in cell behaviour.

    Riento and Ridley (2003) Nat Rev Mol Cell Biol 4(6) : 446-56
    PubMedID: 12778124
  • 3, ROCK inhibitor Y27632 promotes proliferation and diminishes apoptosis of marmoset induced pluripotent stem cells by suppressing expression and activity of caspase 3.

    Wu et al (2016) Theriogenology 85(2) : 302-14
    PubMedID: 26476594
  • 4, Detrimental effect of post Status Epilepticus treatment with ROCK inhibitor Y-27632 in a ... model of temporal lobe epilepsy.

    Kourdougli et al (2015) Front Cell Neurosci. 9 : :413
  • 5, Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity.

    Breitenlechner et al (2003) Structure 11(12) : 1595-607
    PubMedID: 14656443
  • 6, Reprogram or reboot: small molecule approaches for the production of induced pluripotent stem cells and direct cell reprogramming.

    Jung et al (2014) ACS Chem Biol 9(1) : 80-95
    PubMedID: 24245936
  • 7, A ROCK inhibitor permits survival of dissociated human embryonic stem cells.

    Wanatabe et al (2007) Nat Biotechnol 25(6) : 681-6
    PubMedID: 17529971
  • 8,Molecular pathway and cell state responsible for dissociation-induced apoptosis in human pluripotent stem cells.

    Ohgushi et al (2010) Cell Stem Cell 7(2) : 225-39
    PubMedID: 20682448
  • 9, Failure of Y-27632 to improve the culture of adult human adipose-derived stem cells.

    Lamas et al (2015) Stem Cells Cloning 8 : 15-26
    PubMedID: 25609984
  • 10, Effect of Rho-kinase Inhibitor, Y27632, on Porcine Corneal Endothelial Cell Culture, Inflammation and Immune Regulation.

    Lee et al (2016) Ocul Immunol Inflamm 24(5) : 579-93
    PubMedID: 26471144
  • 11, Application of Rho-associated protein kinase (ROCK) inhibitor to human pluripotent stem cells.

    Kurosawa (2012) J Biosci Bioeng. 114(6) : 577-81
    PubMedID: 22898436
  • 12, Novel cryopreservation method for dissociated human embryonic stem cells in the presence of a ROCK inhibitor.

    Martin-Ibañez et al (2008) Hum Reprod. 23(12) : 2744-54
    PubMedID: 18716037
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Reviews

  • Verified customer, University of Louisville

    The Y-27632 is working as expected.