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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Smad2/3 Inhibitor
Luspatercept is a recombinant modified ActRIIB fusion protein that functions as a Smad2/3 inhibitor. It selectively binds to transforming growth factor β (TGF-β) superfamily ligands, including GDF11, thereby inhibiting Smad2/3 signaling. This compound promotes the maturation of erythroid precursors and increases erythrocyte numbers, making it a valuable tool for research into anemia and related erythropoietic disorders. -
Smad3 Inhibitor
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. It significantly inhibits the myofibroblast differentiation of fibroblasts induced by TGF-β1 while leaving the phosphorylation of Smad2 unaffected. This specificity makes SIS3 free base a valuable tool for studying the role of Smad3 in cellular processes associated with fibrosis and other TGF-β1 mediated pathways. -
Syk Inhibitor, NF-κB p65 Inhibitor, TGF-β1/Smad Signaling Inhibitor
Flavanomarein is a potent inhibitor of Syk and NF-κB p65, as well as a modulator of TGF-β1/Smad signaling pathways. This compound exhibits cytoprotective, anti-inflammatory, and antioxidant activities, enhancing AKT phosphorylation while regulating key proteins such as PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2, and ICAD. Flavanomarein also inhibits the nuclear translocation of NF-κB p65 and modulates epithelial-mesenchymal transition (EMT) markers, promoting proliferation in HK-2 cells and protecting neuronal cells from 6-OHDA-induced neurotoxicity. This compound is valuable for research on Parkinson's disease and diabetic nephropathy. -
TGF-β Inhibitor
TGFβ-IN-2 is an orally active inhibitor of TGF-β, targeting its signaling pathways. This compound effectively suppresses TGF-β-induced expression of key proteins such as COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 exhibits significant anti-fibrotic effects in a Bleomycin-induced pulmonary fibrosis model, making it a valuable tool for investigating the mechanisms and potential treatments of pulmonary fibrosis. -
TGF-β1/Smad Signaling Pathway Inhibitor
DGM is a specific inhibitor of the TGF-β1/Smad signaling pathway, exhibiting notable antifibrotic properties. It effectively inhibits the epithelial-mesenchymal transition (EMT) in alveolar epithelial cells, thereby slowing the progression of pulmonary fibrosis in vivo. DGM reduces lung inflammation, enhances lung function, and minimizes extracellular matrix remodeling, making it a valuable tool for research on idiopathic pulmonary fibrosis (IPF) and other EMT-related diseases. -
TGF-β1 Inhibitory Peptide
P17 Peptide is a selective inhibitor of human TGF-β1, functioning by blocking its activity. This peptide is valuable for studying the role of TGF-β1 in various biological processes and disease states, including fibrosis and cancer. Its inhibitory effects facilitate research into therapeutic strategies targeting TGF-β signaling pathways. -
TGF-β1 Inhibitor
DT-6 is a selective inhibitor of TGF-β1, a key regulator of cellular processes related to fibrosis and cancer progression. By inhibiting TGF-β1, DT-6 effectively disrupts M2 macrophage-induced epithelial to mesenchymal transition (EMT) and inhibits the invasive migration of cancer cells. This compound is valuable for research applications focused on cancer biology and related therapeutic interventions. -
TGF-β/Smad/MAPK Inhibitor
TGF-β/Smad-IN-3 is a potent inhibitor of the TGF-β/Smad signaling pathway and MAPK pathway. This compound demonstrates significant anti-pulmonary fibrosis activity by inhibiting collagen deposition resulting from TGF-β1, with an IC50 of 3.21 μM. Additionally, TGF-β/Smad-IN-3 effectively reduces the expression of α-SMA, COL1A1, and FN in TGF-β1-induced CCC-HPF-1 cells, while also significantly reducing cell migration. This reagent is valuable for research focused on pulmonary fibrosis and related fibrosis-related mechanisms. -
TGF-β1 Inhibitor
H-Leu-Ser-Lys-Leu-OH (LSYL) is an inhibitor of TGF-β1 activation, functioning as a latency-associated peptide derived from the amino terminus of LAP. By binding to KRFK, it effectively obstructs the signaling pathway of TGF-β1, thereby mitigating hepatic damage and fibrosis. This compound serves as a valuable tool for research into therapeutic interventions targeting TGF-β1-mediated pathways in fibrotic diseases. -
TGF-β1 Inhibitor
PXS 64 is a selective inhibitor of TGF-β1, targeting the activation of latent transforming growth factor-beta 1. This lipophilic prodrug, a mannose-6-phosphate analogue, demonstrates potent anti-fibrotic activity by attenuating the TGF-β1 signaling pathway in human lung fibroblasts. It effectively reduces the expression of key fibrotic markers including collagen IV, fibronectin, MCP-1, and phospho-Smad2 in renal cells. PXS 64 is applicable in research related to chronic kidney disease, idiopathic pulmonary fibrosis, and dermal scarring, making it a valuable tool for studies of fibrotic disorders. -
PKC/PKA Inhibitor
MDL 27032 is a selective active site-directed inhibitor of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA), exhibiting Ki values of 24 μM and 14.3 μM, respectively. This compound demonstrates significant vasodilatory effects by relaxing vascular smooth muscle. Its properties make MDL 27032 a valuable tool for investigating PKC and PKA-mediated pathways in cardiovascular research and other related studies. -
PKA Inhibitor
Rp-8-Br-cAMPS sodium is a selective inhibitor of Protein Kinase A (PKA) that functions by occupying the cAMP binding sites on the regulatory subunits of PKA type I. This prevents the dissociation and activation of PKA, making it a valuable tool for studying signaling pathways dependent on PKA. Research applications include investigations into tumor biology, retrovirus-induced immune deficiencies, and the regulation of insulin secretion. -
PKA Inhibitor
H-8 dihydrochloride is a reversible, cell-permeable inhibitor of protein kinase A (PKA) that operates through an ATP-competitive mechanism. It effectively modulates PKA activity, making it a valuable tool for investigating cellular signaling pathways. This compound is widely utilized in cancer research and studies focused on metabolic disorders, allowing researchers to elucidate the roles of PKA in various biological contexts. -
PKA Inhibitor
PKI (14-24)amide TFA is a potent inhibitor of protein kinase A (PKA) that effectively blocks cyclic AMP-dependent protein kinase activity in various cellular contexts. This compound demonstrates significant inhibitory action, making it valuable for studies involving PKA-related signaling pathways. Its utilization in research can provide insights into the molecular mechanisms of PKA-mediated processes in health and disease. -
PKA Inhibitor
PKI (14-24)amide is a potent inhibitor of Protein Kinase A (PKA), effectively disrupting the activity of cyclic AMP-dependent protein kinase. This compound has been shown to strongly inhibit PKA activity in cell homogenates, making it a valuable tool for studying PKA-related signaling pathways and their biological implications. Its application in research can facilitate investigations into cellular processes regulated by PKA, contributing to a better understanding of various physiological and pathological conditions. -
PKA Inhibitor
GEM-231 is an 18mer antisense oligonucleotide that specifically targets the mRNA of the PKA-I (RIα regulatory subunit of cAMP-dependent protein kinase type I). This compound has demonstrated the ability to induce cell growth arrest, apoptosis, and differentiation across various cancer cell lines in vitro, as well as in tumor models in vivo. GEM-231 serves as a valuable tool for investigating PKA signaling pathways and their implications in cancer biology. -
PKA Inhibitor
PKI (5-24), amide is a potent inhibitor of cAMP-dependent protein kinase A (PKA), derived from the active region of the heat-stable inhibitor protein. With an inhibition constant (Ki) of 2.3 nM, it effectively disrupts PKA signaling pathways. This reagent is valuable for research applications focusing on PKA-mediated cellular functions and signaling cascades in various biological contexts. -
J-PKA Inhibitor
Aplithianines A is a selective inhibitor of J-PKAcα, exhibiting an IC50 value of 1 μM, while also demonstrating inhibition of wild-type PKA with an IC50 of 84 nM. This compound exerts its inhibitory effects by competitively binding to the ATP pocket of J-PKAcα, thereby affecting its catalytic activity. Aplithianines A is valuable for research applications involving protein kinase signaling pathways and the study of PKA-related cellular processes. -
PKA Inhibitor
PKItide is a potent inhibitor of Protein Kinase A (PKA), exhibiting an IC50 of 0.2 μM for cAMP-dependent PKA. This compound effectively disrupts PKA signaling pathways, making it a valuable tool for studying cellular processes regulated by cAMP. Research applications include investigating the role of PKA in various physiological and pathological conditions, as well as exploring therapeutic strategies targeting PKA-related diseases. -
PKA Inhibitor
Rp-8-Br-cAMPS is a potent inhibitor of protein kinase A (PKA) that functions by occupying the cAMP binding sites on the regulatory subunits of PKA type I. This inhibition prevents the dissociation and activation of PKA, thereby modulating downstream signaling pathways. Rp-8-Br-cAMPS is particularly useful in research applications focused on tumor biology, retrovirus-induced immune deficiency, and the regulation of insulin secretion. -
PKA Inhibitor
GSK466317A is a potent protein kinase A (PKA) inhibitor, exhibiting an IC50 of 12.59 μM. In addition to its primary target, GSK466317A also demonstrates inhibitory activity against GRK1, GRK2, and GRK5, with corresponding IC50 values of 1000 μM, 31.62 μM, and 39.81 μM, respectively. This compound is valuable for research applications involving signal transduction pathways and the study of G protein-coupled receptor (GPCR) functionality. -
PKA/PKC Inhibitor
Protein Kinase Inhibitor 7 is an inhibitor of Protein Kinase A (PKA) and Protein Kinase C (PKC). This compound modulates the autocrine motility factor (AMF) signaling pathway, demonstrating potential applications in cancer research and studies involving cell signaling without influencing overall cell motility. It is a valuable tool for elucidating the roles of PKA and PKC in various biological processes. -
MLCK/PKA Inhibitor
ME 3407 is a myosin light chain kinase (MLCK) and protein kinase A (PKA) inhibitor that disrupts H+-K+-ATPase redistribution. This compound effectively blocks gastric acid secretion and inhibits aminopyrine accumulation by preventing the microsomal-to-apical membrane redistribution of H+-K+-ATPase. ME 3407 demonstrates potential for use in research related to peptic ulcers and other gastrointestinal disorders. -
AKAP-PKA interaction inhibitor
FMP-API-1 is an inhibitor of the A-kinase anchoring protein (AKAP)-PKA interaction. By binding to the allosteric site of protein kinase A (PKA) regulatory subunits, FMP-API-1 enhances PKA activity and promotes the function of aquaporin-2 (AQP2) in PKA-knockout renal cortical collecting duct cell lines (mpkCCD cells). This compound is valuable for investigating nephrogenic diabetes insipidus (NDI) and the underlying mechanisms of renal water transport. -
PKC/PKA Inhibitor
Balanol is a highly selective ATP-competitive inhibitor of Protein Kinase C (PKC) and Protein Kinase A (PKA), demonstrating potent activity against various human PKC isozymes, including α, β-I, β-II, γ, δ, ε, η, and ζ, with IC50 values ranging from 4 to 150 nM. This compound effectively inhibits the phosphorylation of key downstream targets such as cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides, making it a valuable tool for research involving PKC/PKA signaling pathways. -
PKA/AKAP Inhibitor
PKA/AKAP-IN-2 is a non-peptide inhibitor targeting the interaction between protein kinase A (PKA) and A kinase anchoring proteins (AKAP). This compound disrupts the PKA-AKAP binding, providing valuable insights into signaling pathways influenced by cAMP. PKA/AKAP-IN-2 is useful for research into diseases linked to cAMP dysregulation and the broader implications of PKA signaling in cellular processes. -
PKA Inhibitor
4-Cyano-3-methylisoquinoline is a potent protein kinase A (PKA) inhibitor, exhibiting an IC50 at the micromolar range. This compound has demonstrated the ability to reverse morphine tolerance in murine models, highlighting its potential use in pain management research and studies exploring opioid signaling pathways. Its role as a PKA inhibitor makes it a valuable tool for investigating cellular processes regulated by this important kinase. -
PKA/AKAP Inhibitor
PKA/AKAP-IN-1 is a potent non-peptide inhibitor that selectively disrupts the interaction between protein kinase A (PKA) and A-kinase anchoring proteins (AKAP). This compound is valuable for investigating the role of cAMP signaling in various pathological conditions associated with its dysregulation. Research applications include studies on cellular signaling pathways and potential therapeutic interventions in diseases linked to altered PKA/AKAP interactions. -
ROCK2 Inhibitor
ROCK2-IN-12 is a selective ROCK2 inhibitor, demonstrating an IC50 of 7.0 nM for ROCK2 relative to ROCK1. This compound exhibits potent antifibrotic effects by modulating the TGF-β/Smad and ROCK2/STAT3 signaling pathways, effectively reducing collagen deposition and reversing fibrosis in Bleomycin-induced pulmonary fibrosis mouse models. ROCK2-IN-12 is suitable for investigating lung diseases, particularly pulmonary fibrosis. -
ROCK2 Inhibitor
ROCK2-IN-7 is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2). It effectively disrupts ROCK2/pSTAT3 signaling pathways, leading to decreased systemic immune activation and reduced inflammation. This compound is particularly valuable in studies related to autoimmune conditions, such as psoriasis, as it provides insights into the modulation of immune responses and inflammatory processes. -
Smad Inhibitor
(14S,15R)-14-Deoxyoxacyclododecindione is a selective inhibitor of the TGF-β-dependent Smad2/3 and IL-4-dependent STAT6 signaling pathways, exhibiting IC50 values of 90 nM and 20 nM, respectively. This compound has significant potential for applications in cancer research and the study of fibrotic diseases by modulating key signaling events. Its ability to inhibit these pathways makes it a valuable tool for investigating the role of TGF-β and IL-4 in various biological processes. -
Akt/ROCK Inhibitor
Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development. -
TGF-β Inhibitor
TGF-βRI inhibitor 3 is a selective inhibitor of the TGF-β receptor type I (ALK5), designed to effectively disrupt TGF-β signaling pathways. It demonstrates notable inhibitory activity with IC50 values of 0.63 μM against ALK5 and 13 μM against c-Src kinase. This compound is valuable for research applications targeting fibrosis, cancer progression, and other TGF-β-mediated biological processes. -
TGF-beta/Smad Inhibitor
RepSox hydrochloride is a highly selective inhibitor of transforming growth factor-β receptor I (TGF-β-RI) and activin-like kinase 5 (ALK5). It effectively inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. This reagent is valuable for investigating the roles of TGF-β signaling in obesity and metabolic disorders, including type 2 diabetes. -
MAPKAPK2 Inhibitor
MK2-IN-1 is a selective inhibitor of MAPKAPK2 (MK2), exhibiting an IC50 of 0.11 µM. This compound significantly interferes with the phosphorylation of serine residues in Tfcp2l1, with an EC50 of 0.35 µM for phosphorylated HSP27. MK2-IN-1 serves as a valuable tool for studying the role of MK2 in cellular signaling pathways and its implications in various biological processes. -
PKC inhibitor
Bryostatin 1 is a macrolactone isolated from the marine bryozoan, Bugula neritina, that modulates protein kinase C (PKC) activity. Bryostain 1 induces an initial rapid activation and autophosphorylation of PKC that results in the translocation of the PKC enzyme to the membrane. -
EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent. -
ROCK Inhibitor
GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK). -
PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer.
