Catalog No.
Product Name
Application
Product Information
Citations
- Protein Kinase C (19-31), this peptide derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, it was used as protein kinase C substrate peptide for testing the protein kinase C activity.
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Akt inhibitor
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family. -
ROCK inhibitor
H-1152 dihydrochloride, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. -
ROCK inhibitor
Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
ROCK inhibitor
Hydroxyfasudil hydrochloride, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
ROCK activator
Narciclasine is a Rho/Rho kinase/LIM kinase/cofilin signaling pathway activator. -
ROCK2 Inhibitor
SLx-2119 is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM). -
antiviral agent
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst. -
ROCK Inhibitor
RKI-1447 dihydrochloride is a selective inhibitor of Rho-associated kinase (ROCK), exhibiting IC50 values of 14.5 nM and 6.2 nM for ROCK1 and ROCK2, respectively. This compound effectively suppresses the growth of colorectal carcinoma cells while inducing apoptosis, making it a valuable tool for research in cancer biology and therapeutics targeting ROCK signaling pathways. -
ROCK/ERK/GSK/AGC Inhibitor
ROCK-IN-5 (compound I-B-37) is a potent inhibitor of Rho-associated protein kinase (ROCK), as well as ERK, GSK-3, and AGC protein kinases. This compound exhibits significant biological activity in regulating cellular proliferation and has applications in researching cardiac conditions and neurodegenerative diseases. Its broad inhibitory profile makes it a valuable tool for studies aimed at understanding signaling pathways involved in various disease mechanisms. -
PKA Inhibitor
HA-1004 hydrochloride is a selective inhibitor of protein kinase A (PKA), known for its ability to inhibit lipolysis and promote vascular relaxation. In addition to its PKA inhibition, HA-1004 also functions as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein synthesis, impacting smooth muscle and second messenger pathways. This compound serves as a vasodilator, effective in inhibiting the contraction of rabbit aortic strips, and can also antagonize ERK and tyrosine hydroxylase phosphorylation in morphine abstinence models. -
PKA Inhibitor
HA-1004 dihydrochloride is a selective inhibitor of protein kinase A (PKA), demonstrating significant inhibition of lipolysis and induction of vascular relaxation. Additionally, it acts as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase, playing a crucial role in regulating smooth muscle activity and second messenger pathways. This compound serves as a vasodilator, effectively inhibiting contraction in rabbit aortic strips, and also antagonizes ERK and tyrosine hydroxylase phosphorylation in models of morphine abstinence. -
ROCK2 Inhibitor
NRL-1049 dihydrochloride is a selective inhibitor of rho-associated protein kinase 2 (ROCK2), exhibiting an IC50 value of 0.59 μM. This compound demonstrates a remarkable selectivity for ROCK2 over ROCK1, with an IC50 of 26 μM, effectively inhibiting ROCK2 activity. NRL-1049 dihydrochloride has significant potential in research applications focused on the preservation of the blood-brain barrier following acute injury. -
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.
