PKC Activator

1-Stearoyl-2-Arachidonoyl-d₈-sn-Glycerol is the deuterium labeled 1-Stearoyl-2-arachidonoyl-sn-glycerol. 1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity.

(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein increases myotubes Ca²⁺ influx.

1,2-Didecanoyl-sn-glycerol is an analog of the PKC-activating second messenger DAG. Although the biological activities of 1,2-didecanoyl-sn-glycerol have not been well characterized, it is expected to behave similarly to 1,2-dioctanoyl-sn-glycerol.

Kiss2 peptide acetate is the acetate form of Kiss2 pepride (HY-P10256). Kiss2 peptide acetate is a positive regulator of reproduction. Kiss2 peptide acetate binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC₅₀: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)

SC-9 is a PKC activator in the presence of Ca²⁺.

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.

Ingenol 3-monobenzoate (Ingenol 3-benzoate) is a disgust inducing agent. Ingenol 3-monobenzoate can bind to and activate PKC (K_i=0.14 nM), inhibit the gene expression of phosphoenolpyruvate carboxykinase, thereby inhibiting gluconeogenesis, and increasing blood cortisol levels, producing food aversion.

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 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.

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).

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).

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.

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].