PKC Activator

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).

Sapintoxin A is a phorbol ester that can be isolated from the unripe fruits of Sapium indicum.

Kiss2 peptide is a positive regulator of reproduction. Kiss2 peptide 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).

Neuropeptide DF2 is a DRNFLRFamide neuropeptide orignally isolated from crayfish. which enhances transmitter release and stimulates the amplitude of excitatory post-synaptic potentials (EPSP) through the calcium/calmodulin-dependent protein kinase.

Protein Kinase C (530-558), a peptide fragment of protein kinase C (PKC), is a potent PKC activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption.

JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases.

Isosalvianolic acid C is a naturally derived phenolic compound that acts as a signal modulator, antioxidant, and enzyme inhibitor. Isosalvianolic acid C induces the phosphorylation of PLC-γ, IP3R, PKC, and P38, triggering Ca²⁺ mobilization, degranulation, and chemokine release. Isosalvianolic acid C activates MRGPRX2 and its murine homolog MrgprB2, leading to pseudo-allergic reactions in vivo. Isosalvianolic acid C inhibits Cu²⁺-induced LDL peroxidation. Isosalvianolic acid C can be used in studies related to pseudo-allergy, diabetes, and atherosclerosis.

DCPLA-ME (Standard) is the analytical standard of DCPLA-ME (HY-108599A). This product is intended for research and analytical applications. DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.

R 59-022 hydrochloride (Standard) is the analytical standard of R 59-022 (hydrochloride) (HY-107613A). This product is intended for research and analytical applications. 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 K_inase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

Pinoresinol dimethyl ether (Standard) is the analytical standard of Pinoresinol dimethyl ether (HY-N2180). This product is intended for research and analytical applications. Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furanoid lignin. Pinoresinol dimethyl ether can be isolated from Magnolia biondii. Pinoresinol dimethyl ether activates MAPK, PKC, and PKA upstream pathways and inhibits NO levels. Pinoresinol dimethyl ether has neuroprotective activity.

C8-Ceramide (Standard) is the analytical standard of C8-Ceramide (HY-108391). This product is intended for research and analytical applications. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein K_inase (PKC) in vitro.

R59949 (Standard) is the analytical standard of R59949 (HY-108355). This product is intended for research and analytical applications. R59949 is a pan diacylglycerol K_inase (DGK) inhibitor with an IC₅₀ of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein K_inase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.

Daphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.

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