Ask about this productRelated genes to: ROCK2 antibody
- Gene:
- ROCK2 NIH gene
- Name:
- Rho associated coiled-coil containing protein kinase 2
- Previous symbol:
- -
- Synonyms:
- -
- Chromosome:
- 2p25.1
- Locus Type:
- gene with protein product
- Date approved:
- 1999-04-23
- Date modifiied:
- 2016-10-05
Related products to: ROCK2 antibody
Related articles to: ROCK2 antibody
- Recent studies have indicated that the Rho GTPase family and Rho-kinases are associated with psychiatric diseases, such as schizophrenia. Two subtypes of Rho-kinase, Rho-kinases 1 and 2, regulate actin dynamics and mediate neurite outgrowth, spine morphology in neurons, and neurotransmitter release in vitro and ex vivo. However, the precise role of Rho-kinases in neurotransmitter release in vivo remains unclear. To clarify the role of Rho-kinases 1 and 2 in serotonin and dopamine release in the nucleus accumbens (NAc) of mice in vivo, we investigated the effect of a nonselective Rho-kinase inhibitor, fasudil, and a selective Rho-kinase 2 inhibitor, KD025, using an in vivo microdialysis technique. Fasudil perfusion (1-20 μM) into the NAc increased the basal extracellular serotonin level but did not affect dopamine levels, whereas KD025 (10-20 μM) had little effect on basal serotonin and dopamine levels. Notably, fasudil perfusion into the NAc suppressed depolarization-induced serotonin and dopamine release in a dose-dependent manner, whereas KD025 selectively suppressed depolarization-induced serotonin release. Our results suggested that Rho-kinases 1 and 2 are associated with dopamine and serotonin release, respectively, and that both may have significant but distinct roles in the regulation of serotonin and dopamine release in the NAc. - Source: PubMed
Tanaka RinakoZhu WenjunNagai TakuNabeshima ToshitakaKaibuchi KozoOzaki NorioIkesue HiroakiMizoguchi HiroyukiYamada Kiyofumi - Chronic graft-versus-host disease remains a major cause of late morbidity and mortality after allogeneic hematopoietic stem cell transplantation. Conventional prevention and management strategies, heavily reliant on prolonged immunosuppression, are limited by suboptimal efficacy, substantial toxicity, and a failure to address disease heterogeneity. - Source: PubMed
Publication date: 2026/04/22
Liang XiaoliLi DuoJi RuiZhang XinwenWang XiaoqiZhang Xi - - Source: PubMed
Publication date: 2026/04/20
Wang YuLiu WanyingHuang XiaobingXiao Yi - Glioblastoma is the most malignant primary intracranial tumor and is characterized by rapid growth, diffuse invasion, and notable therapeutic resistance. The mesenchymal subtype of glioblastoma multiforme (GBM) is the most aggressive, but the underlying regulatory network of this phenotype has not yet been fully elucidated. - Source: PubMed
Publication date: 2026/03/15
Wang LiangliangZhao FeihuSun YanfeiLiu JilongWang JiazhengWang JianHuang BinLi Xingang - Rho-associated coiled-coil containing kinases (ROCK1 and ROCK2) are central regulators of actin cytoskeleton organization and cell contractility under physiological conditions. Dysregulation of ROCK signaling contributes to aberrant cell migration, invasion, and tissue remodeling, positioning these kinases as attractive therapeutic targets in cancer and fibrotic diseases. In this work, we report the discovery of -acylhydrazone (NAH) derivatives as potent and selective ROCK inhibitors, integrating structure-based virtual screening (SBVS), de novo design, and biological evaluation. Initial hit identification from the LASSBio Chemical Library revealed three inhibitors (LASSBio-1828 (), LASSBio-1829 (), and LASSBio-1919 ()), which guided the rational design of a virtual library of 321 NAH analogues. Docking-based prioritization, synthesis, and SAR exploration yielded compounds with low nanomolar potency, among which LASSBio-2360 (), LASSBio-2380 (), and LASSBio-2382 () exhibited dual ROCK1/2 inhibition (IC values in the 1-15 nM range), while LASSBio-2389 () showed remarkable ROCK2 selectivity (IC = 0.051 μM; 21-fold vs ROCK1 - IC = 1.143 μM) and minimal inhibition of other related kinases at 500 nM. Molecular dynamics simulations demonstrated that stabilizes the DFG-out conformation of ROCK2, providing a structural rationale for isoform selectivity. In vitro studies using MDA-MB-231 triple-negative breast cancer cells confirmed that compounds , , , and inhibit migration more effectively than fasudil and comparably to belumosudil. Altogether, this work identifies NAH as a privileged scaffold for ROCK inhibition, delineates the molecular determinants of ROCK2 selectivity, and highlights new chemical leads for the development of antimetastatic and antifibrotic agents targeting the Rho/ROCK pathway. - Source: PubMed
Publication date: 2026/01/27
Pinheiro Pedro de Sena MurteiraSilva Franco LucasPillpe-Meza Raysa Magalide Jesus Bárbara da Silva MascarenhasMartins Gabrielli Ayumi ItoGouveia Wesley LeandroRodrigues Daniel AlencarAlves Marina AmaralLima Lídia Moreira