PKC
Protein Kinase C Alpha (PKCα) is a serine/threonine kinase involved in diverse cellular processes including proliferation, differentiation, and apoptosis. It plays a critical role in signal transduction pathways downstream of G-protein-coupled receptors and receptor tyrosine kinases[1]. PKCα regulates cell survival and growth through activation of the MAPK/ERK and PI3K/AKT pathways[2]. In cancer, PKCα is often overexpressed and contributes to tumor progression, particularly in breast and prostate cancers[3]. It also modulates vascular smooth muscle contraction and endothelial function, implicating it in cardiovascular diseases. Notably, PKCα exhibits distinct functions compared to other PKC isoforms due to its unique subcellular localization and substrate specificity[4]. Targeting PKCα with selective inhibitors such as Gö6976 has shown therapeutic potential in preclinical models of cancer and inflammatory disorders[5].
References:
- [1]. Lee MJ, et al. Time to HIV rebound after infusion of long-acting broadly neutralising antibodies 3BNC117-LS and 10-1074-LS and analytical treatment interruption (the RIO trial): a double-blind, randomised, placebo-controlled trial. Lancet HIV. 2026 May 27:S2352-3018(26)00059-7. [Content Brief]
- [2]. Wolf S, et al. Selection for Evi1 activation in myelomonocytic leukemia induced by hyperactive signaling through wild-type NRas. Oncogene. 2013 Jun 20;32(25):3028-38. [Content Brief]
- [3]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
- [4]. Kim JY, et al. The induction of STAT1 gene by activating transcription factor 3 contributes to pancreatic beta-cell apoptosis and its dysfunction in streptozotocin-treated mice. Cell Signal. 2010 Nov;22(11):1669-80. [Content Brief]
- [5]. Ciglenecki I, et al. Low sensitivity of the fourth-generation antigen/antibody HIV rapid diagnostic test Determine™ HIV Early Detect for detection of acute HIV infection at the point of care in rural Eswatini: a diagnostic accuracy study. J Int AIDS Soc. 2025 Jul;28(7):e26517. [Content Brief]
All Product Categories
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PKC Related Products (384)
Related Products (384)
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SB2960
0 ImagesCat. No.: HY-181165CAS No.: 3111225-79-4SB2960 is a receptor for activated protein C kinase 1 (RACK1) binder with a human KD of 5.65 μM. SB2960 can promote stress granule (SG) formation and exhibit potent antiviral activity across diverse viral species. SB2960 suppresses viral replication with minimal cytotoxicity by modulating host antiviral immune responses. SB2960 increases the thermal stability of RACK1 and reduces SARS-CoV-2 N protein levels. SB2960 enhances type I interferon (IFN-β) expression and inhibits RIG-I, ISG56, and RANTES expression. SB2960 can be used for the research of virus infection.
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R 59-022 hydrochloride (Standard)
0 ImagesCat. No.: HY-107613ARCAS No.: 93076-98-3Synonyms: DKGI-I hydrochloride (Standard); Diacylglycerol kinase inhibitor I hydrochloride (Standard)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 Kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
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Sotrastaurin (Standard)
0 ImagesSynonyms: AEB071 (Standard)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 Kis 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.
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Ro 31-8830
0 ImagesCat. No.: HY-117610CAS No.: 131848-98-1Synonyms: Ro 32-0432 free base; Bisindolylmaleimide XIRo 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.
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Ro 31-8220 mesylate (Standard)
0 ImagesCat. No.: HY-13866RCAS No.: 138489-18-6Synonyms: Ro 31-8220 methanesulfonate (Standard); Bisindolylmaleimide IX mesylate (Standard)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.
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CMPD101 (Standard)
0 ImagesCat. No.: HY-103045RCAS No.: 865608-11-3CMPD101 (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.
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Bisindolylmaleimide I hydrochloride (Standard)
0 ImagesCat. No.: HY-13867ARCAS No.: 176504-36-2Synonyms: GF109203X hydrochloride (Standard); Go 6850 hydrochloride (Standard)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.
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Phellopterin (Standard)
0 ImagesPhellopterin (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.
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Xaliproden hydrochloride (Standard)
0 ImagesSynonyms: SR57746A (Standard); SR57746 hydrochloride (Standard)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.
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p38 MAPK-IN-11
0 ImagesCat. No.: HY-183530CAS No.: 152121-51-2p38 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.
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(+)-Eudesmin (Standard)
0 ImagesCat. No.: HY-N2180RCAS No.: 29106-36-3Synonyms: (+)-Eudesmine (Standard)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.
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TAS-301 (Standard)
0 ImagesCat. No.: HY-18965RCAS No.: 193620-69-8
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C8-Ceramide (Standard)
0 ImagesCat. No.: HY-108391RCAS No.: 74713-59-0Synonyms: N-Octanoyl-D-erythro-sphingosine (Standard)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 Kinase (PKC) in vitro.
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Safingol hydrochloride
0 ImagesCat. No.: HY-112384ACAS No.: 139755-79-6Synonyms: L-threo-dihydrosphingosine hydrochlorideSafingol hydrochloride is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.
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CGP60474 (Standard)
0 ImagesCat. No.: HY-11009RCAS No.: 164658-13-3CGP60474 (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 Kinase (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.
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3-Methyl-L-tyrosine
0 ImagesCat. No.: HY-W114420CAS No.: 17028-03-43-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.
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HA-100 (Standard)
0 ImagesCat. No.: HY-100984RCAS No.: 84468-24-6HA-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.
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R59949 (Standard)
0 ImagesCat. No.: HY-108355RCAS No.: 120166-69-0R59949 (Standard) is the analytical standard of R59949 (HY-108355). This product is intended for research and analytical applications. R59949 is a pan diacylglycerol Kinase (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 Kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
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Stearoyl-L-carnitine-d3
0 ImagesCat. No.: HY-113202SCAS No.: 1021439-31-5Stearoyl-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.
