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AB120129

Y-27632 dihydrochloride, Rho kinase inhibitor

Y-27632 dihydrochloride, Rho kinase inhibitor

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(2 Reviews)

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(153 Publications)

Y-27632 dihydrochloride (CAS: 129830-38-2)(ab120129) is a cell-permeable, selective Rho kinase (ROCK) inhibitor. Molecular weight (MW) 320.3, Purity >99%.

- Suitable for stem cell maintenance and differentiation assays
- Used as component in 3D growth matrix and brain organoid differentiation media
- Available in multiple sizes to fit your experimental needs. Larger volume format available upon request
- Proven performance: cited in over 150 publications

別名を表示する

CP2D6_HUMAN, CPD6, CYP2D, CYP2D7AP, CYP2D7BP, CYP2D7P2, CYP2D8P2, CYP2DL1, CYPIID6, Cardiolipin activated protein kinase Pak2, Cholesterol 25-hydroxylase, Cytochrome P450 2D6, Cytochrome P450 family 2 subfamily D member 6, Cytochrome P450 family 2 subfamily D polypeptide 6, Cytochrome P450-DB1, Debrisoquine 4-hydroxylase, KIAA0619, KPCE_HUMAN, MGC125656, MGC125657, MGC131603, MGC150606, MGC43611, MGC71074, Microsomal monooxygenase, P450 DB1, P450C2D, PKCE, PKN gamma, PKN2_HUMAN, PRK2, PRKCE, PRKCL2, PRO0435, PRO2042, Pkcea, Protein kinase C epsilon, Protein kinase C epsilon type, Protein kinase C-like 2, Protein kinase N2, Protein-kinase C-related kinase 2, ROCK-I, ROCK1_HUMAN, ROCK2_HUMAN, ROK alpha, Renal carcinoma antigen NY-REN-35, Rho associated coiled coil containing protein kinase 1, Rho associated coiled coil containing protein kinase 2, Rho associated, coiled coil containing protein kinase II, Rho kinase, Rho kinase 2, Rho-alpha kinase, Rho-associated, Rho-associated protein kinase 1, Rho-associated protein kinase 2, Rock II, Rock2m, Rok, Serine/threonine-protein kinase N2, Xenobiotic monooxygenase, coiled-coil-containing protein kinase 1, coiled-coil-containing protein kinase 2, coiled-coil-containing protein kinase I, flavoprotein-linked monooxygenase, nPKC-epsilon, p160 ROCK, p160 ROCK-1, p160 Rhoassociated coiled coil-forming protein kinase, p164 ROCK-2, Y27632

3 Images
Functional Studies - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)
  • FuncS

Unknown

Functional Studies - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)

ab46154 staining VEGF in HeLa cells treated with Y-27632 dihydrochloride (ab120129), by ICC/IF. Decrease in VEGF expression correlates with increased concentration of Y-27632 dihydrochloride, as described in literature.
The cells were incubated at 37°C for 1h in media containing different concentrations of ab120129 (Y-27632 dihydrochloride) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab46154 (5 μg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

Functional Studies - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)
  • FuncS

PubMed

Functional Studies - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)

A : Serum-starved human TM cells were incubated on chamber glass slides coated with recombinant human Gal8 in the presence of the ROCK inhibitor ab120129, at different concentrations. After 2 hr, cells were stained with rhodamine-labeled phalloidin, and cells with robust stress fibers were enumerated. Data are expressed as mean±SEM.

B : Cells were treated with an 120129 (Y27632) at 20 μM, stained with rhodamine-labeled phalloidin, and random fields were photographed. Note that cells treated with ab120129 are not spread and exhibit dendrite-like structures.

Credit : Shiri D et al. PLoS One. 2012; 7(7) : e41958. doi : 10.1371/journal.pone.0044400

Shiri D et al. PLoS One. 2012; 7(7): e41958. doi: 10.1371/journal.pone.0044400 Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

Chemical Structure - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)
  • Chemical Structure

Lab

Chemical Structure - Y-27632 dihydrochloride, Rho kinase inhibitor (AB120129)

2D chemical structure image of ab120129, Y-27632 dihydrochloride, Rho kinase inhibitor

Key facts

CAS番号

129830-38-2

精製度

>99%

製品の状態

Solid

form

分子量

320.3 Da

分子式

C<sub>1</sub><sub>4</sub>H<sub>2</sub><sub>3</sub>Cl<sub>2</sub>N<sub>3</sub>O

PubChem

9901617

由来

Synthetic

溶解性

Available in multiple formatsab144494: Soluble in 1 of ml water to give specified mM/ml concentration; ab120129: Soluble in water to 100 mM and in DMSO to 100mM.

化学名

(1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride

生物学的記述

Selective Rho kinase inhibitor.

Canonical smiles

CC(C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl

Isomeric smiles

C[C@H](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl

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

IUPAC名

4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide;dihydrochloride

製品の詳細

Y-27632 is a research tool with a wide variety of biological effects, mainly used in the field of stem cell research for maintenance and differentiation. Commonly used as 3D growth matrix component; also a component of brain organoid differentiation media.

How others have used Y-27632 in their research:

Maintenance of tissue culture of iPSCs; 10 μM Y-27632 for 24 hr;  Montefiori et al (2018)
Reprogramming of breast cancer cells to induced progenitor-like cells (iPLs) ; 2 μM Y27632 ; Yuan et al (2018)
Differentiation - Y-27632 enables human embryonic stem cells to survive and differentiate into cortical and basal telencephalic progenitors; Watanabe et al (2007)

*Also available in simple stock solutions (ab144494) - add 1 ml of water to get an exact, ready-to-use concentration.

出荷温度及び保存条件

出荷温度
Ambient - Can Ship with Ice
短期保存温度
+4°C
長期保存温度
+4°C
保管に関する情報
Store under desiccating conditions|The product can be stored for up to 2 years

Need more advice on solubility, usage and handling? Please visit our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Refer to SDS for further information.

補足情報

This supplementary information is collated from multiple sources and compiled automatically.

ROCK1 and ROCK2 also known as Rho-associated coiled-coil containing protein kinases 1 and 2 are serine/threonine kinases with molecular masses of approximately 158 kDa and 160 kDa respectively. These kinases play an essential role in cell structures and functions like contraction motility and adhesion. ROCK1 and ROCK2 express in various tissues including the brain heart and skeletal muscle where they regulate actin cytoskeleton dynamics. ROCK1 and ROCK2 function as effectors for small GTPase RhoA modulating the cytoskeleton through phosphorylation of different substrates.
Biological function summary

ROCK1 and ROCK2 contribute significantly to the regulation of smooth muscle contraction actin cytoskeleton organization and cellular migration. They exist in their complex forms and primarily act by phosphorylating downstream target proteins which leads to changes in cell shape and movement. Their activity influences various cellular processes such as apoptotic regulation and tissue rigidity which are fundamental in development and homeostasis. Increased levels or activity of ROCKs link to pathological changes including vascular diseases and cancer progression.

Pathways

ROCK1 and ROCK2 are key components of the Rho/ROCK signaling pathway and the integrin-mediated signaling pathway. These pathways are vital for cellular activities like adhesion migration and proliferation. They often interact with other proteins such as LIM kinase and myosin phosphatase modulating actin-myosin contractility. The Rho/ROCK pathway in particular act as a hub for signal transduction connecting extracellular cues to intracellular responses. This pathway regulates many physiological responses by affecting various cellular substrates and signaling molecules.

ROCK1 and ROCK2 show significant involvement in cardiovascular diseases and cancer. Dysregulation of ROCK activity contributes to hypertension by affecting vascular smooth muscle contraction while aberrant ROCK signaling often results in increased cell migration and invasion in cancerous cells. In hypertension targeting ROCKs can help reduce blood pressure as ROCK inhibitors like dihydrochloride are used therapeutically. Moreover in cancer ROCK1 and ROCK2 interact with proteins such as focal adhesion kinase which lead to enhanced tumor cell migration and metastasis highlighting potential therapeutic targets.

製品プロトコール

文献 (153)

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