PKC Activator

Methyl arachidonate is a protein kinase C activator and also an orally active substrate that undergoes esterase-mediated hydrolysis. Methyl arachidonate indirectly activates protein kinase C via eicosanoid metabolites generated through the arachidonic acid metabolic pathway, exerting effects via cyclooxygenase products at low concentrations and via lipoxygenase products at high concentrations. Methyl arachidonate can be used in studies related to lipodystrophy.

MRS2768 tetrasodium salt is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 tetrasodium salt activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 tetrasodium salt inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 tetrasodium salt activates eNOS to increase NO secretion in endothelial cells. MRS2768 tetrasodium salt drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 tetrasodium salt exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 tetrasodium salt can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a K_i of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion.

2-(1-Piperazinyl)pyrimidine (Standard) is the analytical standard of 2-(1-Piperazinyl)pyrimidine. This product is intended for research and analytical applications. 2-(1-Piperazinyl)pyrimidine is the major metabolite of Tandospirone (HY-14558).

AJH-836 is an activator of Munc13-1 and PKC ε/α (K_d: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases.

Chrysosplenol C is a type of flavonoid compound. Chrysosplenol C selectively activates cardiac myosin ATPase, with its EC₅₀ being 45 µM. Chrysosplenol C enhances the release of intracellular calcium ions by activating protein kinase C (PKC), thereby increasing the contractility of rat ventricular muscle cells. Chrysosplenol C can be used in the research of heart failure.

1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA₁₀) and activates protein kinase C (PKC).

Junicedric acid is a diterpenoid compound that can be isolated from the resin of the Araucaria araucana tree. Junicedric acid exerts neuroprotective activity by increasing intracellular calcium levels in hippocampal neurons, activating PKC and calcium/calmodulin-dependent protein kinase (CaMKII), and preventing Amyloid-β oligomer-induced synaptic protein loss, apoptosis, and long-term potentiation (LTP) inhibition. Junicedric acid can be used in the study of the pathological mechanisms of neurodegenerative diseases such as Alzheimer's disease.

PKC(85–92),Myristoylated is a cell permeable myristic acid conjugated PKC peptide activator that enhances NO release in cultured human umbilical vein endothelial cells (HUVECs).

Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

PKC activator-1 (compound 26) is a PKC activator (K_i = 1.2 nM). PKC activator-1 exhibits cytotoxicity towards various cancer cells. PKC activator-1 is commonly used in cancer research.

MRS2768 is a potent, selective, and metabolically stable P2Y₂ receptor agonist with an EC₅₀ of 1.89 μM for the human P2Y₂ receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y₂-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.

Gnidimacrin is a protein kinase C (PKC) activator. Gnidimacrin inhibits cell growth of human leukemias, stomach cancers and non-small cell lung cancers in vitro, and shows activity against murine leukemias and solid tumors in vivo. Gnidimacrin can be used for leukemias, stomach cancers and non-small cell lung cancers research.

Decursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities[4].

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) (GMP) is Phorbol 12,13-dibutyrate (HY-18985) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Phorbol 12,13-dibutyrate is a PKC activator and a potent skin tumor promoter.

DCP-LA (Standard) is the analytical standard of DCP-LA. This product is intended for research and analytical applications. DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis[1][2][3].

L-α-Phosphatidylinositol-4,5-bisphosphate ammonium is a key signaling lipid. L-α-Phosphatidylinositol-4,5-bisphosphate ammonium is an activator of PKC in the presence of calcium ions and phospholipid serine. L-α-Phosphatidylinositol-4,5-bisphosphate ammonium is also an antagonist of the KIR3.4 (ATP-sensitive potassium, KATP) channel. L-α-Phosphatidylinositol-4,5-bisphosphate ammonium can be used in research related to signal transduction, ion channel regulation, and membrane transport.

MGF24 is a modified protease-resistant MGF derivative. MGF24 protects dopaminergic neurons from 6-Hydroxydopamine (6-OHDA) (HY-113028)-induced apoptosis by inducing Heme oxygenase-1 (HO-1). MGF24 activates PKC-ε, which in turn activates Nrf2, up-regulating HO-1. MGF24 has neuroprotective activity and reduces myocardial infarct size in sheep models of myocardial ischemia. MGF24 can be used for neurological diseases like stroke, nerve injury and amyotrophic lateral sclerosis research.

Decursinol angelate (Standard) is the analytical standard of Decursinol angelate. This product is intended for research and analytical applications. Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.

pTH-Related Protein (1-40) (human, mouse, rat) stimulates calcium uptake in rat intestinal cells through PTHR1 receptor and PKCα/β signaling pathways. pTH-Related Protein (1-40) up-regulates parathyroid hormone 1 receptor (PTHR1) protein, four transcellular calcium transporters, potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium Exchanger 1 (NCX1) and plasma membrane calcium ATPase 1 (PMCA1).