Catalog No.
Product Name
Application
Product Information
Citations
-
CaMKII inhibitor
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
-
CaMK-II inhibitor
KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II, with Ki of 370 nM.- Kazuki Yuasa, .et al. , Sci Rep, 2018, 8: 9037 PMID: 29899565
-
CaM kinase II inhibitor
KN-93 is an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase.- Margherita Zaupa, .et al. , Neuron, 2024, Apr 3;112(7):1150-1164 PMID: 38295792
- Christian E Coleman, .et al. , Arch Microbiol, 2022, Jul 24;204(8):519 PMID: 35871646
-
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
CaMK1D Inhibitor
CS640 is a selective inhibitor of calmodulin-dependent kinase 1D (CaMK1D) with additional activity against several other kinases, including CaMK1B, CaMK1A, and MEK5, demonstrating IC50 values of 8 nM, 3 nM, 1 nM, and 25 nM, respectively. This compound effectively inhibits Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, making it valuable for studies on tau pathology. While CS640 does not provide protective effects against Aβ-induced neurotoxicity in primary mouse cortical neurons, it is useful for research focusing on the mechanisms of Alzheimer's disease. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
CaMK II Inhibitor
Lavendustin C is a selective inhibitor of calcium/calmodulin-dependent kinase II (CaMK II), exhibiting an IC50 of 0.2 µM. In addition to its primary mechanism, Lavendustin C also targets epidermal growth factor receptor (EGFR)-associated tyrosine kinase with an IC50 of 0.012 µM and pp60c-src(+) kinase at an IC50 of 0.5 µM. This compound is valuable in research applications focused on signaling pathways involving CaMK II and its associated kinases, aiding in the study of various cellular processes and potential therapeutic interventions. -
CaMKK2 Inhibitor
CC-3240 is a highly selective inhibitor of CaMKK2, exhibiting a potent inhibitory effect with an IC50 of 9 nM. This molecular glue degrader, developed from CC-8977, effectively disrupts the function of CaMKK2, making it a valuable tool for investigations into calcium and calcium/calmodulin-dependent signaling pathways. CC-3240 is particularly useful in research applications aimed at exploring the role of CaMKK2 in cellular processes and disease states. -
mGluR1/CaMKIIα Activator
FO-4-15 is an mGluR1/CaMKIIα activator that demonstrates neuroprotective effects against oxidative stress, specifically H2O2, in human neuroblastoma SH-SY5Y cells. This compound enhances cognitive function in mouse models of Alzheimer’s disease by engaging the mGluR1/CaMKIIα signaling pathway, leading to a reduction in amyloid-beta accumulation, hyperphosphorylated Tau, and synaptic damage. It serves as a valuable tool for investigating mechanisms of neuroprotection and cognitive impairment in neurodegenerative diseases. -
CaMKK2 Inhibitor
CaMKK2-IN-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) with an IC50 of 7 nM. This compound displays high ligand efficiency, making it a valuable tool for investigating the role of CaMKK2 in cellular signaling pathways. Its application in research includes studies on metabolism, cancer, and neurological disorders where the modulation of CaMKK2 activity may provide insights into therapeutic interventions. -
CAMKK2 Inhibitor
SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2), exhibiting an IC50 of 30 nM. This compound effectively inhibits AMPK phosphorylation in C4-2 cells with an IC50 of 1.6 μM. SGC-CAMKK2-1 serves as a valuable chemical probe for investigating the role of CAMKK2 in various biological processes and pathways related to cellular energy regulation and metabolism. -
Calcineurin Inhibitor
Mevalonolactone is a sesquiterpene lactone that acts as a calcineurin inhibitor, demonstrating inhibitory activity with an IC50 value of 134.29 μM against p-Nitrophenyl phosphate. This compound is primarily used in research exploring cellular signaling pathways, immune response modulation, and potential therapeutic applications for disorders involving calcineurin activity. Its ability to inhibit calcineurin makes it valuable for investigations into T cell activation and cytokine production. -
Calcineurin NFAT Inhibitor
NFAT Inhibitor-2 is a selective inhibitor of calcineurin, targeting the calcium-regulated NFAT signaling pathway. This compound demonstrates significant potential in research related to inflammatory diseases, autoimmune disorders, cardiovascular conditions, neurodegenerative diseases, and disorders characterized by uncontrolled cell proliferation or differentiation. Additionally, NFAT Inhibitor-2 may provide insights into angiogenesis-related diseases, allergies, anaphylaxis, and alopecia. -
Antioxidant Agent
6,4'-Dihydroxy-7-methoxyflavanone is a flavonoid with notable antioxidant properties. This compound effectively inhibits receptor activators of nuclear factor kappa-B ligand (RANKL) induced osteoclastogenesis, making it a valuable tool in bone health research. Additionally, it exhibits anti-inflammatory and neuroprotective effects, supporting its utility in studies related to osteoporosis and neurodegenerative diseases. -
CaMK1D Inhibitor
CS587 is a selective inhibitor of Calcium/calmodulin-dependent protein kinase 1D (CaMK1D), demonstrating neurocytotoxic effects at concentrations of 10 μM. This compound modulates neuronal cell sensitivity to amyloid-beta (Aβ) oligomer toxicity, making it a valuable tool for studying neurodegenerative disorders and related cellular pathways. Its specificity and mechanism of action position CS587 as a significant reagent for research into neuronal health and disease mechanisms. -
Calmodulin Antagonist
W-13 hydrochloride is a calmodulin antagonist that effectively disrupts calmodulin-mediated signaling pathways. This compound has demonstrated the ability to inhibit the growth of Tamoxifen-resistant human breast cancer cells, making it a valuable tool for cancer research. Its mechanism of action provides insights into potential therapeutic strategies for overcoming resistance in breast cancer treatment. -
CaMKIIδ Inhibitor
CaMKIIδ-IN-1 is a potent inhibitor of calcium/calmodulin-dependent protein kinase II delta (CaMKIIδ) with an IC50 of 12 nM. This pyrimidine-based compound is valuable for studying the role of CaMKIIδ in various cellular processes, including synaptic plasticity and cardiac function. Its selective inhibition makes it a useful tool for investigating the biochemical pathways regulated by CaMKIIδ in both physiological and pathological contexts. -
CaMKK Inhibitor
TIM-063 is a selective, cell-permeable CaMKK inhibitor that functions as an ATP-competitive antagonist, specifically targeting the catalytic domain of CaMKK. It exhibits Ki values of 0.35 μM for CaMKKα and 0.2 μM for CaMKKβ, with corresponding IC50 values of 0.63 μM and 0.96 μM. This compound is useful for exploring CaMKK-mediated signaling pathways and evaluating its potential therapeutic applications in various cellular models. -
CaMKIIα Inhibitor
CaMKIIα-IN-1 is an orally active inhibitor of calcium/calmodulin-dependent protein kinase II alpha (CaMKIIα), exhibiting a dissociation constant (KD) of 219 nM for the wild-type hub. This compound demonstrates good metabolic stability, making it suitable for in vivo studies. It can be utilized in research focused on CaMKIIα-mediated pathways, with applications in understanding neurological diseases and cellular signaling mechanisms. -
Diversity-Oriented Synthesis
BRD0418 is a diversity-oriented synthesis molecule that targets tribbles pseudokinase 1, influencing its expression. This compound has been shown to modulate lipoprotein metabolism, facilitating the transition from fat production to clearance. BRD0418 is valuable in research applications related to coronary artery disease (CAD), providing insights into metabolic regulation and cardiovascular health. -
CaMKIIα Ligand
PTCA is a potent ligand for calcium/calmodulin-dependent protein kinase II alpha (CaMKIIα), exhibiting a pKi value of 7.2. This compound effectively modulates CaMKIIα activity, making it valuable for research into calcium signaling pathways and their implications in neuronal functions and synaptic plasticity. Its use in biochemical assays facilitates the exploration of CaMKIIα's role in various physiological and pathological processes. -
CaMKIIα Modulator
Ph-HTBA is a selective modulator of CaMKIIα, exhibiting a high binding affinity with a Kd value of 757 nM. This compound effectively penetrates the blood-brain barrier, making it suitable for studying neurological conditions. Its applications include research into ischemia and neurodegenerative disorders, offering potential insights into therapeutic interventions for these diseases. -
CaMK Substrate
Calmodulin Dependent Protein Kinase Substrate is a synthetic peptide designed as a substrate for calmodulin-dependent protein kinases (CaMKs) that are activated by calcium ions (Ca2+) and calmodulin (CaM). This substrate is crucial for studying the phosphorylation activity of CaMKs and aids in understanding their role in various cellular signaling pathways. It is relevant for research applications in signal transduction and regulatory mechanisms in calcium signaling. -
CaMKII Substrate
Autocamtide-3 is a selective substrate for Ca2+/calmodulin-dependent kinase II (CaMKII), characterized by its 13-amino-acid sequence that includes the phosphorylatable residue Thr287. This peptide serves as a valuable tool for studying the activation and regulation of CaMKII in various biological contexts. Its application in research encompasses investigations into calcium signaling, neuronal function, and cardiac physiology. -
CaMKIIα inhibitor
HOCPCA is a selective inhibitor of CaMKIIα, a key regulator of calcium-dependent signaling pathways. This compound exhibits neuroprotective properties, enhancing sensorimotor functions and promoting hippocampal neuronal activity following experimental stroke in murine models. It effectively modulates abnormal CaMKII signaling, normalizes Thr286 autophosphorylation post-ischemia, and downregulates specific active CaMKII fragments associated with ischemic conditions. Additionally, HOCPCA demonstrates superior binding affinity to the GHB site, alongside excellent blood-brain barrier permeability, making it a valuable tool for research into neuroprotection and cognitive function. -
CaMKII Inhibitor
CaMKII-IN-3 is a potent inhibitor of Calcium/Calmodulin-dependent protein kinase II (CaMKII), demonstrating an IC50 of less than 10 nM. This compound is valuable in research focused on the role of CaMKII in cardiac function and related heart diseases. Its application may provide insights into disease mechanisms and potential therapeutic strategies. -
CaMKII Inhibitor
Protein kinase inhibitor 8 (Compound CK59) is a selective inhibitor of calmodulin-dependent protein kinase II (CaMKII). This compound effectively reduces cytotoxicity induced by perfluorooctane sulfonic acid (PFOS) and mitigates the downregulation of GLT-1 expression, leading to decreased neuronal damage. Protein kinase inhibitor 8 is a valuable tool for research into neurodegenerative diseases and the molecular mechanisms underlying neuronal stress responses. -
CaMK Substrate
Calmodulin Dependent Protein Kinase Substrate Analog is a synthetic peptide designed as a substrate for calmodulin-dependent protein kinases (CaMK). As a Ca2+- and calmodulin-dependent substrate, it facilitates the study of CaMK activity and regulation in cellular signaling pathways. This analog is valuable for investigating phosphorylation processes and the role of CaMK in various biological systems, making it a useful tool in biochemical and pharmacological research. -
CaMKIIα Degrader
CaMKIIα-PHOTAC is a photochemically targeted chimera designed to selectively degrade Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Upon exposure to specific wavelengths of light, this compound facilitates the ubiquitination and subsequent degradation of CaMKIIα through the endogenous proteasome pathway. Its application has demonstrated a reduction in synaptic function, notably diminishing the amplitude of evoked field excitatory postsynaptic potentials in the mouse hippocampus, thereby implicating its role in the modulation of long-term potentiation and memory processes in dendritic regions. -
PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
PKD inhibitor
CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively. -
PKD1 inhibitor
CID797718 is a structural analog of CID755673 (Adooq Catalog No. A13804). It was a 10-time less potent PKD1 inhibitor with an IC50 value of 7.0 +/-0.8 uM. -
PKD Inhibitor
CRT-0066101, potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively). -
CaMKK inhibitor
STO-609 is a cell-permeable inhibitor of calcium/calmodulin-dependent kinase kinases (CaMKK) isoforms CaMKKα and CaMKKβ (Ki = 80 and 15 ng/ml, respectively). -
calmodulin inhibitor
Zaldaride maleate (CGS-9343B) is a potent and selective inhibitor of calmodulin. -
CaMKII inhibitor
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM. -
CaMK antagonist
Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM. -
CaMKII inhibitor
KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). -
CaMK Substrate
Syntide 2 is a substrate peptide for calcium/calmodulin-dependent protein kinase II (CaMKII) that demonstrates selective inhibition of the gibberellin (GA) signaling pathway. By targeting this pathway, Syntide 2 facilitates the investigation of mechanisms underlying plant hormone responses while preserving the activity of other regulatory events, such as those mediated by abscisic acid. This reagent is valuable for studies related to cellular signaling and hormone regulation in plant biology.
