ROCK2
ROCK2 (Rho-associated coiled-coil-containing protein kinase 2) is a serine/threonine kinase that functions as a major downstream effector of Rho GTPases and regulates cytokinesis, smooth muscle contraction, actin stress fiber formation, focal adhesion dynamics, and transcriptional responses linked to cytoskeletal remodeling[1][2]. Mechanistically, ROCK2 promotes actomyosin contractility through signaling networks that control actin organization, cell morphology, migration, proliferation, adhesion, and inflammatory responses, placing it at the center of cytoskeleton-dependent cellular regulation[3][5]. Because these processes govern tissue homeostasis and cellular adaptation, dysregulated ROCK signaling has been implicated in cardiovascular, neurodegenerative, inflammatory, and cancer-associated pathologies[3][2]. In experimental disease models, ROCK2 has been identified as an important regulator of neuronal survival, axonal stability after injury, and regenerative responses, supporting its utility for studying neurodegeneration and neural repair mechanisms[4]. Compared with the closely related isoform ROCK1, ROCK2 shares high homology within the kinase domain but exhibits distinct tissue distribution and isoform-specific biological functions, highlighting the importance of discriminating ROCK2-dependent signaling from broader ROCK activity in mechanistic studies[3][2]. For experimental applications, pharmacological inhibition of ROCK signaling is widely used to interrogate cytoskeletal regulation and disease-associated pathways, and the development of isoform-selective inhibitors has increased interest in defining ROCK2-specific functions with greater precision[2]>.
References:
- [1]. ROCK2 gene information from NCBI.
- [2]. Wikipedia.
- [3]. Julian L, et al. Rho-associated coiled-coil containing kinases (ROCK): structure, regulation, and functions. Small GTPases. 2014;5:e29846. [Content Brief]
- [4]. Wikipedia.
- [5]. Koch JC, et al. ROCK2 is a major regulator of axonal degeneration, neuronal death and axonal regeneration in the CNS. Cell Death Dis. 2014 May 15;5(5):e1225. [Content Brief]
- [6]. Loirand G. Rho Kinases in Health and Disease: From Basic Science to Translational Research. Pharmacol Rev. 2015;67(4):1074-1095.
All Product Categories
-
ROCK2 Related Products (76)
Related Products (76)
-
Antibodies (1)
-
SB-772077B dihydrochloride
0 ImagesSB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases.
-
LX7101
0 ImagesLX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research.
-
PT109
0 ImagesPT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.
-
Verosudil
0 ImagesSynonyms: AR-12286Verosudil (AR-12286) is a ROCK inhibitor. Verosudil has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil increases trabecular outflow capacity to reduce intraocular pressure. Verosudil is useful in the study of glaucoma and ocular hypertension.
-
NRL-1049
0 ImagesSynonyms: BA-1049 free baseNRL-1049 (BA-1049 (free base)) is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations.
-
Sovesudil hydrochloride
0 ImagesSynonyms: PHP-201 hydrochloride; AMA0076 hydrochlorideSovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia.
