Catalog No.
Product Name
Application
Product Information
Citations
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LIMK Inhibitor
LIMK-IN-1 is a potent inhibitor of LIM-Kinase (LIMK), exhibiting IC50 values of 0.5 nM for LIMK1 and 0.9 nM for LIMK2. This compound is primarily utilized in research related to ocular hypertension and associated glaucoma, contributing to studies aimed at understanding the role of LIMK in these conditions. Its high specificity and efficacy make it a valuable tool for investigating the molecular pathways involved in ocular diseases. -
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. -
CK1/CDK1/CDK5 Inhibitor
(R)-DRF053 dihydrochloride is a selective inhibitor of casein kinases 1 (CK1), CDK1/cyclin B, and CDK5/p25, exhibiting IC50 values of 14 nM, 220 nM, and 80 nM, respectively. This compound effectively inhibits the CK1-mediated generation of amyloid-beta in cellular models, making it valuable for research into neurodegenerative diseases and cellular signaling pathways. Its specificity and potency position it as a suitable reagent for investigating the roles of these kinases in various biological processes. -
CK1/CHK1 Inhibitor
MRT00033659 is a selective inhibitor targeting casein kinase 1 (CK1) and checkpoint kinase 1 (CHK1), with IC50 values of 0.9 μM and 0.23 μM, respectively. As a pyrazolo-pyridine analogue, MRT00033659 activates the p53 signaling pathway and causes destabilization of E2F-1. This compound is valuable for research investigating cell cycle regulation, DNA damage response, and therapeutic strategies in cancer biology. -
Chk2 Inhibitor
(E/Z)-Chk2-IN-1 is a potent and selective inhibitor of the cell cycle kinase Chk2, with an IC50 of 8 nM. This compound demonstrates minimal inhibitory activity against other kinases, including CK1δ, MEK1, and PKCα/βⅡ, with IC50 values greater than 89 nM. (E/Z)-Chk2-IN-1 is suitable for research applications in cancer biology, particularly in elucidating the role of Chk2 in cell cycle regulation and tumorigenesis. -
CDK8 Inhibitor
P162-0948 is a selective inhibitor of Cyclin-Dependent Kinase 8 (CDK8), demonstrating an IC50 value of 50.4 nM. This compound effectively reduces cell migration and downregulates the expression of epithelial-mesenchymal transition (EMT)-related proteins in A549 human alveolar epithelial cells. Additionally, P162-0948 inhibits Smad phosphorylation, indicating its potential to disrupt the TGF-β/Smad signaling pathway. This makes P162-0948 a valuable tool for research focused on pulmonary fibrosis and related pathways. -
Nur77 Modulator
Nur77 modulator 3 is an effective modulator of Nur77, targeting the regulation of hepatic stellate cell (HSC) activation. This compound induces Nur77 expression, leading to decreased ECM deposition and enhanced autophagic flux that is dependent on Nur77. Additionally, it significantly inhibits the mTORC1 signaling pathway, resulting in reduced inflammation and amelioration of hepatic fibrosis in vivo. Nur77 modulator 3 is particularly useful for studies related to liver pathology and fibrosis research. -
CDK8 Inhibitor
CDK8-IN-11 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 46 nM. This compound effectively inhibits the WNT/β-catenin signaling pathway, making it a valuable tool for investigating the molecular mechanisms underlying oncogenesis. CDK8-IN-11 is primarily utilized in research related to colon cancer, contributing to the development of targeted therapeutic strategies. -
CDK6/9 Inhibitor
CDK6/9-IN-2 is a potent dual inhibitor of cyclin-dependent kinases CDK6 and CDK9, with reported IC50 values of 15 nM and 22 nM, respectively. This compound exhibits selectivity for CDK2, CDK8, and CDK11. CDK6/9-IN-2 effectively inhibits the proliferation of HaCaT cells stimulated by IFN-γ and TNF-α, while also suppressing the STAT3 signaling pathway and the expression of inflammatory factors. Its ability to alleviate psoriatic dermatitis makes CDK6/9-IN-2 valuable for research in psoriasis and related inflammatory conditions. -
KRAS Inhibitor
BBO-11818 is a highly selective non-covalent pan-KRAS inhibitor, targeting the Switch-II/Helix 3 pocket with an IC50 range of 28-120 nM. This compound effectively disrupts the KRAS:RAF1 interaction, leading to inhibition of the MAPK signaling pathway, resulting in significant anti-tumor effects. It demonstrates the ability to not only inhibit cell proliferation and induce apoptosis but also promote tumor regression in xenograft models. BBO-11818 is particularly valuable in research focused on KRAS mutation-related malignancies, including pancreatic cancer, non-small cell lung cancer, and colorectal cancer, and exhibits synergistic effects when used in combination with other therapeutic agents. -
CDK Inhibitor
AS2863619 free base is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 0.61 nM and 4.28 nM, respectively. This compound drives the conversion of antigen-specific effector and memory T cells into Foxp3+ regulatory T (Treg) cells, thereby offering potential therapeutic approaches for various immunological conditions. The inhibition of CDK8/19 by AS2863619 enhances STAT5 activation, leading to the upregulation of the Foxp3 gene and promoting Treg cell development. -
CDK3 Inhibitor
Vanicoside B is a potent inhibitor of cyclin-dependent kinase 8 (CDK8), derived from the herb Persicaria dissitiflora. This compound demonstrates significant anti-tumor activity by disrupting CDK8-mediated signaling pathways and reducing the levels of proteins associated with epithelial-mesenchymal transition. As a result, Vanicoside B induces cell cycle arrest and apoptosis, making it a valuable reagent for cancer research and therapeutic investigations targeting CDK8 pathways. -
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. -
CDK8/19 Inhibitor
CDK8/19-IN-2 is a potent and orally active inhibitor of cyclin-dependent kinases 8 and 19, exhibiting IC50 values of 2.08 nM and 2.49 nM, respectively. This compound is crucial for research focusing on acute myeloid leukemia (AML), breast cancer, and lymphoma, where inhibition of CDK8 and CDK19 can influence tumor proliferation and survival. Its selectivity and efficacy make it a valuable tool in studying the role of these kinases in various oncogenic pathways. -
PLK Inhibitor
Poloxipan is a pan-specific inhibitor targeting polo-like kinases (PLKs), specifically interfering with the Polo-box domain at the C-terminus. It demonstrates IC50 values of 3.2 μM, 1.7 μM, and 3.0 μM against PLK-1, PLK-2, and PLK-3, respectively. Additionally, Poloxipan inhibits various phospho-tyrosine binding domains, including the forkhead-associated domain of CHK-2 and the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1). This compound is valuable for applications in cancer research, particularly in studies involving PLK pathways and associated cellular processes. -
CDK8/19 Inhibitor
CDK8-IN-16 is a potent dual inhibitor of cyclin-dependent kinases 8 and 19, demonstrating IC50 values of 5.1 nM and 5.6 nM, respectively. This compound effectively inhibits phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cells and modulates the WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cells. CDK8-IN-16 exhibits favorable pharmacokinetic properties, including an oral bioavailability of 57% in rat models, making it a valuable tool for research in cancer biology and therapeutic development. -
KRAS G12D Inhibitor
KRAS G12D-IN-30 is a selective inhibitor of the KRAS G12D mutant, targeting the KRAS oncogene involved in various cancers. By inhibiting the activation of the downstream MAPK signaling cascade, specifically the Raf1-MEK-ERK pathway, this compound provides valuable insights into oncogenic signaling mechanisms. KRAS G12D-IN-30 is suitable for cancer research applications, particularly in studies focusing on KRAS-driven tumor biology and therapeutic strategies. -
KRAS Inhibitor
KRAS inhibitor-27 is a specific inhibitor targeting KRAS mutations, particularly effective against KRAS G12D and G12V variants. It demonstrates potent biological activity with IC50 values of 378 nM and 0.6 nM in AsPC-1 and SW620 cell lines, respectively, while showing a markedly reduced effect on wildtype KRAS HT-29 cells (IC50 3230 nM). This compound effectively inhibits ERK phosphorylation and reduces DUSP4 expression, thereby disrupting the MAPK signaling pathway. KRAS inhibitor-27 is valuable for research applications focusing on cancer biology and therapeutic strategies against KRAS-driven tumors.
