PKC

Bisindolylmaleimide I (hydrochloride) (Standard) is the analytical standard of Bisindolylmaleimide I (hydrochloride). This product is intended for research and analytical applications. Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.

Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

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.

p38 MAPK-IN-11 is a CSBP (p38 MAPK) kinase inhibitor with IC₅₀ values of 0.15 μM (binding activity) and 0.21 μM (inhibitory activity). p38 MAPK-IN-11 shows weak inhibitory activity against PKCα kinase, with an IC₅₀ of 7.6 μM. p38 MAPK-IN-11 inhibits the production of IL-1. p38 MAPK-IN-11 also acts as a β-lactam antibiotic potentiator, but has no antibacterial activity itself.

R8605 is an inhibitor for PKC with an IC₅₀ of 65 μM for PKC in rat brain. R8605 inhibits calcium/phospholipid-independent phosphorylation of protamine with IC₅₀ of 70 μM and 100 μM. R8605 can be used in cancer research.

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.

TAS-301 (Standard) is the analytical standard of TAS-301. This product is intended for research and analytical applications. TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors.

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.

Safingol hydrochloride is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.

Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC₅₀ of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC₅₀s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.

CGP60474 (Standard) is the analytical standard of CGP60474 (HY-11009). This product is intended for research and analytical applications. CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent K_inase (CDK) inhibitor (IC₅₀ values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.

3-Methyl-L-tyrosine is a derivative of L-Tyrosine (HY-N0473). Structurally, 3-Methyl-L-tyrosine features a methyl modification at the third position of the aromatic ring of L-Tyrosine. As a substrate for the protein tyrosine kinase Csk, 3-Methyl-L-tyrosine's relative catalytic efficiency (kcat/Km) is 38% of L-Tyrosine, indicating that the methyl modification impacts the processing efficiency of Gsk significantly. 3-Methyl-L-tyrosine helps to deepen the understanding of Gsk's molecular recognition mechanisms of its substrates, which is crucial for developing specific inhibitors targeting Gsk.

HA-100 (Standard) is the analytical standard of HA-100 (HY-100984). This product is intended for research and analytical applications. HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.

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.

Stearoyl-L-carnitine-d₃ is the deuterium labeled Stearoylcarnitine. Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2.

BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice.

Mitoxantrone-d₈ (hydrochloride) (Mitozantrone-d₈ (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction.

Ruboxistaurin hydrochloride (Standard) is the analytical standard of Ruboxistaurin hydrochloride (HY-10195B). This product is intended for research and analytical applications. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC₅₀ of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC₅₀ of 5.9 nM.