NEWS ｜ 07 April 2024

WIKIMOLE—Y-27632 & Y-27632 2HCl

By TargetMol

 

 

Y-27632, catalog number T1870, is a selective inhibitor of ROCK-I and ROCK-II, exhibiting oral bioavailability and ATP competitiveness. Y-27632 can also inhibit apoptosis of dissociation-induced mouse prostate stem cells or progenitor cells, commonly used in stem cell research and organoid culture.

  

Y-27632 2HCl, catalog number T1725, also known as Y-27632 dihydrochloride or trans-4-[(R)-1-aminoethyl]-N-(4-pyridyl)cyclohexanecarboxamide dihydrochloride, is the dihydrochloride salt form of Y-27632, exerting the same inhibitory effects as Y-27632.

 

Background

ROCK (Rho-associated coiled-coil-containing protein kinase) is a type of protein kinase associated with Rho GTPases, primarily acting as downstream effectors of the Rho family. ROCK plays a crucial role inside cells, regulating various biological processes, including: influencing cell adhesion to the extracellular matrix, participating in cell division and proliferation, controlling cell migration and movement, and affecting cell contraction and morphological changes. In cell signaling pathways, ROCK is regulated upstream by Rho GTPases, particularly RhoA. Downstream, ROCK is involved in the phosphorylation of various signaling molecules.

ROCK inhibitors have potential therapeutic applications in various diseases, including cancer, glaucoma, asthma, erectile dysfunction, insulin resistance, neurodegeneration, osteoporosis, renal failure, fibrosis, and graft-versus-host disease.

 

Application

Y-27632/Y-27632 2HCl, as a ROCK inhibitor, has significant applications not only in diseases like cancer but also in organoid culture and stem cell research, contributing to the maintenance of cell survival and functionality, thus holding crucial value in various fields.

Common applications:

1) Cryopreservation of stem cells: Y-27632 helps prevent dissociation-related cell apoptosis during the low-temperature preservation of stem cells and enhances cell viability post-thaw.

2) Pancreatic ductal adenocarcinoma organoid culture: Y-27632 serves as a supplement to the culture medium.

3) Mouse embryonic stem cells: Y-27632 inhibits the Rho kinase (Rho) in these cells.

4) Human embryonic stem cells and induced pluripotent stem cells (iPSCs): Y-27632 inhibits Rho-associated protein kinase (ROCK).

These diverse applications highlight the versatility and importance of Y-27632/Y-27632 2HCl in various research settings, promising advancements in cell biology and regenerative medicine.

Reference

[1] Feng, Y. et al. (2016) Rho kinase (ROCK) inhibitors and their therapeutic potential. J. Med. Chem. 59, 2269–2300

[2] Zanin-Zhorov, A. and Blazar, B.R. (2021) ROCK2, a critical regulator of immune modulation and fibrosis has emerged as a therapeutic target in chronic graft-versus-host disease. Clin. Immunol. 230, 108823.

[3] Barcelo J, Samain R, Sanz-Moreno V. Preclinical to clinical utility of ROCK inhibitors in cancer. Trends Cancer. 2023;9(3):250-263. doi:10.1016/j.trecan.2022.12.001

[4] Wu Y, Shu J, He C, et al. ROCK inhibitor Y27632 promotes proliferation and diminishes apoptosis of marmoset induced pluripotent stem cells by suppressing expression and activity of caspase 3. Theriogenology. 2016;85(2):302-314. doi:10.1016/j.theriogenology.2015.09.020

[5] Zhu Y, Wang L, Yin F, Yu Y, Wang Y, Liu H, Wang H, Sun N, Liu H, Qin J. A hollow fiber system for simple generation of human brain organoids. Integr Biol (Camb). 2017 Sep 18;9(9):774-781. doi: 10.1039/c7ib00080d. PMID: 28795726.