Catalog No.
Product Name
Application
Product Information
Citations
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ROCK Inhibitor
Zelasudil is a selective inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), demonstrating significant anti-fibrotic activity. This small molecule enhances immunomodulatory responses in metastatic pancreatic tumors, promoting increased infiltration of CD8+ and CD4+ T cells while reducing FOXP3+ regulatory T cells at the tumor periphery. Zelasudil shows potential for advancing research in pancreatic ductal adenocarcinoma and related therapeutic strategies. -
ROCK/NET Inhibitor
Netarsudil functions as a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). This compound effectively reduces intraocular pressure through ROCK inhibition, promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, facilitating aqueous humor outflow while simultaneously decreasing aqueous humor production via NET inhibition. Netarsudil is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK2 Inhibitor
Belumosudil mesylate is a selective inhibitor of the Rho-associated kinase 2 (ROCK2), demonstrating an IC50 of 105 nM for ROCK2 and 24 µM for ROCK1. This compound exhibits significant anti-fibrotic properties, making it valuable for research in fibrosis-related pathways and diseases. Belumosudil mesylate is applicable in studies aimed at understanding the role of ROCK signaling in various physiological and pathological processes. -
ROCK Inhibitor
SAR407899 is a selective and potent ROCK inhibitor that acts competitively with ATP, exhibiting an IC50 of 135 nM for ROCK-2 and Kis of 36 nM in human and 41 nM in rat ROCK-2. This compound demonstrates stable inhibition of migrasome formation and is valuable for research into cellular migration and related processes. Its application in studies of ROCK signaling pathways may enhance the understanding of various physiological and pathological conditions. -
ROCK/NET Inhibitor
Netarsudil dimesylate is a potent inhibitor of Rho-associated kinases (ROCK I and ROCK II) and also serves as a reversible inhibitor of the norepinephrine transporter (NET). It effectively reduces intraocular pressure through ROCK inhibition, leading to the relaxation of trabecular meshwork cells and dilation of episcleral veins, which facilitates aqueous humor outflow, while simultaneously inhibiting NET to diminish aqueous humor production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK Inhibitor
Sovesudil is a potent Rho kinase (ROCK) inhibitor that functions through ATP-competitive mechanisms, exhibiting IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively lowers intraocular pressure (IOP) while minimizing the risk of hyperemia, making it a valuable compound for ocular research and potential therapeutic applications in glaucoma treatment and other related conditions. -
ROCK Inhibitor
Verosudil is a potent Rho-associated protein kinase (ROCK) inhibitor, demonstrating robust inhibitory activity against both ROCK1 and ROCK2 with a Ki value of 2 nM. Its relatively lower selectivity for other kinases such as PKA, PKCT, MRCKA, and CAMK2A provides additional research avenues. Verosudil enhances trabecular outflow capacity, making it a valuable reagent in studies targeting intraocular pressure reduction. This compound is particularly relevant for research focused on glaucoma and ocular hypertension. -
ROCK Inhibitor
3-(4-Pyridyl)indole is a selective Rho-kinase (ROCK) inhibitor, exhibiting an IC50 value of 25 μM. This compound is known to effectively inhibit cellular blebbing and promote the dissolution of actin stress fibers, making it a valuable reagent for studying wound healing mechanisms and cytoskeletal dynamics in various biological research applications. -
ROCK Inhibitor
GSK269962A hydrochloride is a potent ROCK inhibitor that selectively targets Rho-associated coiled-coil kinase 1 (ROCK1) and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively. It exhibits significant anti-inflammatory and vasodilatory properties, making it valuable in research applications focused on vascular biology, cardiovascular diseases, and inflammatory conditions. This compound provides a useful tool for elucidating the role of ROCK signaling in various biological processes. -
ROCK Inhibitor
CAY10746 is a selective inhibitor of Rho-associated protein kinase (ROCK), demonstrating potent inhibitory activity against ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. This compound is particularly relevant for research into diabetic retinopathy (DR) and other conditions associated with abnormal vascular function. Its ability to modulate ROCK activity makes it a valuable tool in studying cellular pathways involved in inflammation and tissue remodeling. -
ROCK/PKC Inhibitor
(rac)-AR-13503 is a potent inhibitor of Rho-associated protein kinase (ROCK) and protein kinase C (PKC). It plays a significant role in regulating angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. Additionally, (rac)-AR-13503 has demonstrated the ability to inhibit aberrant neovascularization in the oxygen-induced retinopathy (OIR) model in mice, making it a valuable tool for research in ocular disorders and vascular biology. -
ROCK Inhibitor
Rho-Kinase-IN-2 is a selective inhibitor of Rho Kinase (ROCK) with an IC50 value of 3 nM for ROCK2. This orally active and CNS-permeable compound is significant for investigating the role of ROCK in neurodegenerative disorders, particularly Huntington's disease. Its potent inhibition of this pathway makes it a valuable tool for exploring therapeutic strategies targeting ROCK activity in relevant biological models. -
ROCK Inhibitor
Sovesudil hydrochloride is a highly selective Rho kinase (ROCK) inhibitor that competitively binds to ATP, demonstrating IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively reduces intraocular pressure (IOP) and is noteworthy for its ability to do so without causing hyperemia. This compound is utilized in research focused on glaucoma and other ocular conditions linked to elevated IOP. -
ROCK2 Inhibitor
ROCK2-IN-6 hydrochloride is a selective inhibitor of Rho-associated protein kinase 2 (ROCK2). It modulates ROCK2 activity, making it a valuable tool for studying disorders associated with ROCK signaling, including autoimmune diseases and inflammation. This compound is ideal for research aimed at understanding the role of ROCK2 in various biological processes and therapeutic interventions. -
ROCK2 Inhibitor
ROCK2-IN-8 is an orally active inhibitor of Rho-associated protein kinase 2 (ROCK2) with an IC50 of 7.2 nM. This compound is valuable in studies investigating aqueous humor outflow in porcine eyes, as well as the phosphorylation of myosin light chain. Its specificity for ROCK2 makes it a useful tool in exploring the roles of this kinase in various biological processes. -
ROCK1 Inhibitor
GSK-25 is a potent and selective inhibitor of ROCK1, demonstrating an IC50 of 7 nM. This compound exhibits excellent selectivity against a diverse panel of 31 kinases, with over 100-fold selectivity compared to RSK1 (IC50 = 398 nM) and p70S6K (IC50 = 1 µM). GSK-25 is also characterized by its inhibitory effects on specific cytochrome P450 enzymes, with IC50 values of 2.5 µM, 5.2 µM, and 2.5 µM for CYP2C9, CYP2D6, and CYP3A4, respectively. This makes GSK-25 suitable for research applications focused on cell signaling and pharmacological studies involving the ROCK pathway. -
ROCK1 Inhibitor
ROCK1-IN-1 is a selective ROCK1 inhibitor with a Ki value of 540 nM. This compound is utilized in research focused on hypertension, glaucoma, and erectile dysfunction by modulating the Rho-associated protein kinase pathway. Its inhibition of ROCK1 activity provides insight into various physiological processes and potential therapeutic interventions for related disorders. -
ROCK2 Inhibitor
NRL-1049 is a selective inhibitor of ROCK2, demonstrating an IC50 of 0.59 µM for ROCK2 and 26 µM for ROCK1. This compound effectively reduces Lysophosphatidic acid-induced ROCK activation in endothelial cells and has shown potential in animal models by decreasing lesion volume and hemorrhagic transformation associated with cavernous angiomas. Additionally, NRL-1049 preserves the blood-brain barrier, suppresses seizure activity following brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice, making it a valuable tool for research into neurological disorders and vascular pathologies. -
ROCK Inhibitor
ROCK-IN-1 is a highly selective inhibitor of Rho-associated protein kinase (ROCK), demonstrating an IC50 of 1.2 nM specifically for ROCK2. This compound is valuable for studying the role of ROCK in cellular processes such as cytoskeletal dynamics, apoptosis, and smooth muscle contraction. ROCK-IN-1 is particularly useful in investigations related to cardiovascular diseases, cancer research, and neurological disorders. -
ROCK Inhibitor
Rhodblock 6 is a selective Rho kinase (ROCK) inhibitor that targets the phosphorylation of myosin regulatory light chain (MRLC), impacting its localization within cells. By modulating ROCK activity, this compound plays a critical role in the regulation of cytoskeletal dynamics, making it valuable for research applications involving cellular movement, morphology, and signal transduction pathways. Rhodblock 6 is instrumental in studies focused on cancer metastasis, cardiovascular diseases, and neurological disorders. -
RhoA/ROCK Inhibitor
Fasudil hydrochloride semihydrate is a nonspecific inhibitor of RhoA and Rho-associated protein kinase (ROCK), exhibiting a Ki value of 0.33 μM for ROCK1. It shows inhibitory effects on various protein kinases, demonstrating IC50 values of 0.158 μM for ROCK2, and higher values for PKA, PKC, and PKG. Additionally, Fasudil acts as a potent antagonist of calcium channels and displays vasodilatory properties, making it relevant in studies of cardiovascular function and cellular signaling pathways. -
ROCK Inhibitor
Verosudil hydrochloride is a potent ROCK inhibitor, exhibiting strong inhibitory activity against both ROCK1 and ROCK2, with a Ki of 2 nM. It shows lower selectivity for other kinases, including PKA and CAM2A. By increasing trabecular outflow capacity, Verosudil hydrochloride effectively reduces intraocular pressure. This compound is particularly valuable for research focused on glaucoma and ocular hypertension. -
ROCK2 Inhibitor
BIPM is a potent inhibitor of ROCK2, a key regulator of cytoskeletal dynamics. This compound has been shown to significantly influence neurite length, enhance cell migration, and alter the formation of actin stress fibers. BIPM is valuable in research focused on cancer metastasis and is instrumental in elucidating mechanisms of cellular movement and morphology. -
ROCK1/ROCK2 Inhibitor
LASSBio-2382 is a dual inhibitor of ROCK1 and ROCK2, exhibiting IC50 values of 0.005 μM and 0.003 μM, respectively. This compound effectively diminishes the viability and migratory capacity of cancer cells, making it a valuable tool for investigating aggressive cancer types. Its specific application includes research focused on triple-negative breast cancer, facilitating the study of cellular mechanisms and potential therapeutic strategies. -
ROCK2 Inhibitor
ROCK2-IN-6 is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2), targeting the ROCK signaling pathway. This compound demonstrates potent inhibition of ROCK2 activity, making it valuable for the study of ROCK-mediated diseases, including autoimmune disorders and inflammation. Its application in research provides insights into the molecular mechanisms underlying these conditions, aiding the development of potential therapeutic strategies. -
ROCK Inhibitor
Y-33075 hydrochloride is a selective inhibitor of the Rho-associated protein kinase (ROCK). It exhibits enhanced potency compared to its predecessor, Y-27632, with an IC50 of 3.6 nM. This compound is utilized in research to elucidate the role of ROCK in various biological processes, including cellular motility, proliferation, and apoptosis. Its application spans studies in cancer, cardiovascular diseases, and neurodegenerative disorders. -
ROCK Inhibitor
ROCK-IN-32 is a potent inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), exhibiting an IC50 value of 11 nM. This compound is utilized in research focusing on cardiovascular diseases, cancer, and inflammatory processes. ROCK-IN-32 modulates signaling pathways influenced by ROCK2, making it a valuable tool for investigating the physiological and pathological roles of this kinase in various biological contexts. -
ROCK/GRK Inhibitor
GSK317354A is an inhibitor of Rho-associated protein kinase (ROCK) and G protein-coupled receptor kinase (GRK). This compound exhibits potential therapeutic effects in the context of heart failure and Parkinson's disease, facilitating investigations into its role in modulating signaling pathways associated with these conditions. Researchers can utilize GSK317354A to explore its biological activities and implications for treatment strategies. -
ROCK Inhibitor
ROCK-IN-7 is a selective inhibitor of Rho-associated coiled-coil containing protein kinase (ROCK). This compound demonstrates significant inhibitory activity towards ROCK, making it a valuable tool for investigating its role in ocular diseases, including glaucoma and retinal disorders. Researchers can utilize ROCK-IN-7 to explore therapeutic strategies and molecular mechanisms underlying these conditions. -
ROCK Inhibitor
ROCK-IN-8 is a potent Rho-associated protein kinase (ROCK) inhibitor, exhibiting an IC50 value of less than 100 nM. This compound demonstrates significant anti-inflammatory activity, making it suitable for studies related to various inflammatory conditions. ROCK-IN-8 is particularly relevant for research focused on respiratory and gastrointestinal diseases, contributing to the understanding of the underlying mechanisms of these conditions. -
ROCK2 Inhibitor
Desisopropyle-belumosudil is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2). This compound exhibits significant biological activity in the regulation of glucose metabolism and has demonstrated potential benefits in mitigating obesity and enhancing insulin sensitivity. It is a valuable tool for researchers investigating metabolic disorders, including diabetes and obesity. -
ROCK Inhibitor
ROCK-IN-9 is a selective inhibitor of Rho-associated protein kinase (ROCK). This compound exhibits cytotoxic effects in HepG2 cells with an IC50 value of 40.8 μM. Additionally, ROCK-IN-9 demonstrates favorable pharmacokinetic properties in murine models, indicating significant in vivo exposure and oral bioavailability at lower doses. Its profile makes it a valuable reagent for research focused on cancer biology and signaling pathways associated with ROCK inhibition. -
ROCK Inhibitor
ROCK-IN-10 is a highly selective inhibitor of Rho-associated protein kinases (ROCK1 and ROCK2), exhibiting IC50 values of 6 nM and 4 nM, respectively. This compound demonstrates over 100-fold selectivity for ROCK over other kinases, making it an invaluable tool for research applications related to cellular signaling, cytoskeletal dynamics, and the study of various pathological conditions, including cancer and cardiovascular diseases. Researchers can utilize ROCK-IN-10 to investigate the role of ROCK in cellular processes and to explore potential therapeutic strategies targeting these kinases. -
ROCK Inhibitor
SB772077B is a selective inhibitor of Rho-associated protein kinase (ROCK), primarily targeting the RhoA/ROCK signaling pathway. This compound exhibits anti-inflammatory properties and enhances aqueous outflow facility, making it relevant for research in glaucoma. Additionally, SB772077B reduces mRNA levels of β-catenin and proteins associated with fibrosis, such as vinculin, fibronectin, collagen 1A, and vimentin. Furthermore, it demonstrates vasodilatory effects and lowers both pulmonary and systemic blood pressure, contributing to its utility in studies related to pulmonary hypertensive disorders. -
ROCK Inhibitor
ROCK-IN-D1 is a potent and selective inhibitor of Rho-associated protein kinase (ROCK). It effectively modulates ROCK activity, leading to decreased downstream phosphorylation events. This compound is valuable for research focused on cellular signaling pathways, vascular biology, and potential therapeutic applications in cancer and cardiovascular diseases. Researchers can leverage ROCK-IN-D1 to elucidate the role of ROCK in various physiological and pathological processes. -
ROCK2 Inhibitor
ROCK2-IN-5 is a selective inhibitor of Rho-associated protein kinase 2 (ROCK2), designed to modulate various cellular pathways implicated in neurodegenerative disorders. This compound exhibits a multitarget profile, integrating structural features from the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 shows promise in the investigation of amyotrophic lateral sclerosis (ALS), particularly concerning SOD1 mutations, by potentially mitigating cellular stress responses and neuroinflammation associated with the disease. -
ROCK Inhibitor
5-Nitro-1H-indazole-3-carbonitrile is a selective Rho kinase (ROCK) inhibitor, exhibiting an IC50 of 6.67 μM for ROCK-I. This compound demonstrates significant capacity to reduce norepinephrine-induced transient contractions and inhibits calcium-induced contractions in endothelial-denuded rat vascular rings. While it possesses vasorelaxant properties, it is important to note its associated toxicity. 5-Nitro-1H-indazole-3-carbonitrile is relevant for research in cardiovascular diseases, particularly in studies of hypertension. -
ROCK2 Inhibitor
LASSBio-2389 is a selective inhibitor of Rho-associated protein kinase 2 (ROCK2) with an IC50 of 0.051 μM and demonstrates lower potency against ROCK1 with an IC50 of 1.143 μM. This compound effectively reduces the viability of MDA-MB-231 cells and inhibits cell migration, making it a valuable tool for investigating the pathophysiology of triple-negative breast cancer. Its targeted action on ROCK2 positions LASSBio-2389 as a significant reagent in cancer research applications focused on aggressive tumor behaviors. -
ROCK Inhibitor
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK), a key regulator of various cellular functions. This compound exhibits tumor anti-metastatic activity, making it a valuable tool in cancer research. WF-536 is suitable for studies exploring the mechanisms of metastasis and the development of targeted cancer therapies. -
ROCK2 Inhibitor
ROCK2-IN-14 is a selective inhibitor of ROCK2, exhibiting an IC50 of 4.8 nM and 212-fold selectivity over ROCK1. This compound inhibits the ROCK2/S100A9 signaling pathway, leading to downregulation of S100A9 expression, inhibition of NM2 phosphorylation, and restoration of cytoskeletal abnormalities. It demonstrates significant anti-inflammatory effects, including the reduction of cytokines such as IgE, TNF-α, IL-6, and TSLP, and is effective in mitigating ear thickening in mouse models of atopic dermatitis. ROCK2-IN-14 is suitable for studies focused on inflammation and skin disorders. -
ROCK Inhibitor
ROCK-IN-11 is a potent inhibitor of Rho-associated protein kinases ROCK1 and ROCK2, exhibiting an IC50 of ≤ 5 μM. This compound effectively modulates cellular signaling pathways involved in various biological processes, making it a valuable tool in cancer research. Additionally, ROCK-IN-11 can be used to explore therapeutic strategies targeting cell migration, proliferation, and apoptosis. -
ROCK2 Inhibitor
ROCK-IN-6 is a potent and selective inhibitor of ROCK2, exhibiting an IC50 of 2.19 nM. This compound serves as a valuable tool for investigating the role of ROCK2 in various biological processes, particularly in the context of glaucoma and retinal diseases. ROCK-IN-6 is ideal for studies exploring cellular signaling pathways and therapeutic interventions in ocular health. -
ROCK Inhibitor
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine is a selective inhibitor of Rho-associated protein kinase (ROCK), exhibiting IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. This compound demonstrates significant cytotoxic activity against human prostate cancer PC-3 cells, with an IC50 value of 0.16 μM. Its efficacy in inhibiting kinase activity makes it a valuable tool for research in cancer therapeutics and related signaling pathways. -
ROCK Inhibitor
ROCK-IN-D2 is a potent and selective inhibitor of Rho-associated protein kinase (ROCK). This compound exhibits significant biological activity by blocking ROCK-mediated signaling pathways, which are implicated in various cellular processes, including cytoskeletal rearrangement and cell migration. ROCK-IN-D2 is primarily utilized in research applications related to cancer biology, cardiovascular diseases, and neurodegenerative disorders, facilitating the study of ROCK's role in these pathologies. -
ROCK Inhibitor
ROCK-IN-4 is a selective inhibitor of Rho-associated protein kinase (ROCK), exhibiting the capacity to maintain nitric oxide releasing ability. This compound effectively reversibly depolymerizes F-actin and inhibits mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 is valuable for research related to glaucoma and ocular hypertension, making it a critical tool for investigating cellular mechanisms involved in these conditions. -
ROCK Inhibitor
OXA-06 is a potent ROCK (Rho-associated protein kinase) inhibitor that demonstrates significant antitumor activity. It disrupts cell migration and inhibits MYPT1 phosphorylation in PANC-1 cells, making it a valuable tool for cancer research. This compound can be utilized in studies focusing on the modulation of cellular dynamics and therapeutic strategies for pancreatic cancer. -
ROCK Inhibitor
Ripasudil free base is a selective inhibitor of Rho-associated protein kinase (ROCK), demonstrating IC50 values of 19 nM for ROCK2 and 51 nM for ROCK1. This compound exhibits significant biological activity in modulating cellular processes such as migration and proliferation, making it valuable in research focused on fibrosis, cancer, and cardiovascular diseases. Ripasudil free base is an important tool for studies investigating the role of ROCK signaling in various physiological and pathological contexts. -
ROCK Inhibitor
CMPD101 hydrochloride is a membrane-permeable inhibitor targeting Rho-associated kinase 2 (ROCK-2), G protein-coupled receptor kinase 2 (GRK2), and GRK3, with IC50 values of 1.4 μM, 18 nM, and 5.4 nM, respectively. This small-molecule compound also inhibits protein kinase C alpha (PKCα) at an IC50 of 8.1 μM. CMPD101 hydrochloride is useful in research focused on cell signaling, smooth muscle contraction, and potential therapeutic applications in cardiovascular and neurological disorders. -
RhoA/ROCK Inhibitor
Fasudil mesylate is a potent RhoA/ROCK inhibitor with a Ki value of 0.33 μM for ROCK1 and IC50 values of 0.158 μM for ROCK2, along with notable inhibition of PKA, PKC, and PKG. This orally active compound also acts as a calcium channel antagonist and vasodilator, demonstrating significant potential in cardiovascular research and the study of cellular signaling pathways. Its diverse inhibitory effects make Fasudil mesylate a valuable tool for investigating RhoA/ROCK-related biological processes. -
LIM/ROCK/PKA Inhibitor
LX7101 monohydrochloride is a potent inhibitor of LIM-kinase, ROCK, and PKA, exhibiting IC50 values of 24 nM, 1.6 nM, 10 nM, and <1 nM for LIMK1, LIMK2, ROCK2, and PKA, respectively. This compound demonstrates significant selectivity for LIMK2 with an IC50 of 4.3 nM in contrast to 32 nM for LIMK1 at 2 μM ATP. LX7101 monohydrochloride is valuable for research into ocular hypertension and associated glaucoma, providing insights into potential therapeutic strategies targeting these pathways.
