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
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ROCK2 Related Products (76)
Related Products (76)
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Antibodies (1)
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LIMK-IN-1
0 ImagesLIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. LIMK-IN-1 can be used for ocular hypertension and associated glaucoma research.
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Glycyl H-1152 hydrochloride
0 ImagesGlycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.
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DJ4
0 ImagesDJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer.
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Fasudil dihydrochloride
0 ImagesSynonyms: HA-1077 dihydrochloride; AT-877 dihydrochlorideFasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
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ROCK2-IN-12
0 ImagesROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0 nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research.
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ROCK/HDAC-IN-2
0 ImagesCat. No.: HY-172177ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).
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Fasudil hydrochloride semihydrate
0 ImagesCat. No.: HY-10341BCAS No.: 186694-02-0Synonyms: HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrateFasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator.
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ROCK/HDAC-IN-1
0 ImagesCat. No.: HY-168650ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity.
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Verosudil hydrochloride
0 ImagesCat. No.: HY-16758ACAS No.: 1414854-44-6Synonyms: AR-12286 hydrochlorideVerosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension.
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ROCK2-IN-9
0 ImagesCat. No.: HY-162798ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC50=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research.
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LASSBio-2382
0 ImagesCat. No.: HY-181582CAS No.: 2487752-24-7
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ROCK2-IN-7
0 ImagesCat. No.: HY-149700CAS No.: 3000541-95-4
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ROCK2-IN-13
0 ImagesCat. No.: HY-179498ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.
