PKC Inhibitor

LY 379196 is a PKC-β inhibitor (IC₅₀: 50 nM and 30 nM for PKC βI and βII respectively). LY 379196 inhibits the VEGF, IGF-1 and bFGF-induced proliferation of bovine retinal microvascular endothelial cells (BREC). LY 379196 is an antiproliferatory agentfor proliferative retinopathy.

PKC-IN-5 (Compound PKCe2054) is a PKC inhibitor. PKC-IN-5 prevents the interaction between PKCe and its adaptor protein RACK2.

Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.

Sotrastaurin (Standard) is the analytical standard of Sotrastaurin. This product is intended for research and analytical applications. Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.

Ro 31-8830 is an orally active, potent and selective inhibitor of protein kinase C with anti-inflammatory activity. Ro 31-8830 is promising for research of inflammatory disorders.

Ro 31-8220 mesylate (Standard) is the analytical standard of Ro 31-8220 mesylate (HY-13866). This product is intended for research and analytical applications. Ro 31-8220 mesylate is a potent PKC inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Ro 31-8220 mesylate can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.

CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.

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.

FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27 (HY-101059). This product is intended for research and analytical applications. FGIN-1-27 is a blood-brain barrier-penetrant TSPO ligand with a K_i value of 5 nM. FGIN 1-27 inhibits PKC-β, PKA/CREB, p38/ERK MAPK, MITF, tyrosinase, TRP-1, and TRP-2, thereby inhibiting melanogenesis and pigmentation. FGIN-1-27 alleviates X-ray radiation-induced astrocyte mitochondrial hyperfunction, reduces ROS and superoxide production, inhibits excessive activation of A1-type astrocytes, downregulates GFAP and C3 protein expression, and restores astrocyte proliferative capacity. FGIN-1-27 produces anticonvulsant effects in normal mice; in diazepam-withdrawn mice, the brain MDR pathway becomes subsensitive, and the anticonvulsant activity disappears. FGIN-1-27 attenuates pigmentation in zebrafish embryos and ameliorates UVB-induced skin pigmentation in guinea pigs. FGIN-1-27 directly stimulates testicular Leydig cells while upregulating luteinizing hormone levels, causing an acute increase in serum testosterone in male rats. FGIN 1-27 can be used for research related to hyperpigmentation, epilepsy, brain injury, and other diseases.

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.

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.

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.

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.

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.