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 (386)
Related Products (386)
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Spisulosine-d3
0 ImagesSynonyms: ES-285-d3Spisulosine-d3 (ES-285-d3) is deuterium labeled Spisulosine (HY-13626). Spisulosine is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation. Spisulosine induces apoptosis in PC-3 and LNCaP cells.
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Methyl arachidonate
0 ImagesSynonyms: Arachidonic acid methyl esterMethyl 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.
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Bisindolylmaleimide I (Standard)
0 ImagesCat. No.: HY-13867RCAS No.: 133052-90-1Synonyms: GF109203X (Standard); Go 6850 (Standard)Bisindolylmaleimide I (Standard) is the analytical standard of Bisindolylmaleimide I. This product is intended for research and analytical applications. Bisindolylmaleimide I (GF109203X) 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 is also a GSK-3 inhibitor.
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Midostaurin (Standard)
0 ImagesSynonyms: PKC412 (Standard); CGP 41251 (Standard)Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
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Fasudil mesylate
0 ImagesCat. No.: HY-10341DCAS No.: 1001206-62-7Synonyms: HA-1077 mesylate; AT-877 mesylateFasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca2+ channel antagonist and vasodilator.
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Mitoxantrone hydrochloride liposome
0 ImagesCat. No.: HY-185372Synonyms: Liposomal mitoxantroneMitoxantrone hydrochloride liposome is a liposome-encapsulated Mitoxantrone hydrochloride (HY-13502A) (a topoisomerase II inhibitor). Compared to regular Mitoxantrone hydrochloride, Mitoxantrone hydrochloride liposome enhances antitumor activity and prolongs drug circulation time in the body.
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Forskolin (GMP)
0 ImagesCat. No.: HY-15371GCAS No.: 66575-29-9Synonyms: Coleonol (GMP); Colforsin (GMP); HL 362 (GMP)Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin (GMP) is also an inducer of intracellular cAMP formation. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy.
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Ruboxistaurin-d6 hydrochloride
0 ImagesCat. No.: HY-10195BSCAS No.: 1794767-04-6Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. 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.
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Mitoxantrone diacetate
0 ImagesCat. No.: HY-13502BCAS No.: 70711-41-0Synonyms: Mitozantrone diacetate; NSC 301739 diacetateMitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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Fasudil hydrochloride semihydrate
0 ImagesCat. No.: HY-10341BCAS No.: 186694-02-0Synonyms: HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrateFasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator.
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β-N-methylamino-L-alanine hydrochloride (Standard)
0 ImagesSynonyms: BMAA hydrochloride (Standard)Clenbuterol (Standard) is the analytical standard of Clenbuterol. This product is intended for research and analytical applications. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM. Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator.
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Calphostin B
0 ImagesCat. No.: HY-N19702CAS No.: 124824-06-2Calphostin B is a protein kinase C (PKC) inhibitor with an IC50 of 1.04 μM in rats and an IC50 of 22.9 μM for bovine cyclic adenosine monophosphate-dependent protein kinase (PKA). Calphostin B bears aromatic structures at positions C-14 and C-17, which accounts for its higher selectivity for PKC over PKA. Calphostin B can be used in studies related to human cervical cancer and human breast cancer.
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PKC-IN-4
0 ImagesCat. No.: HY-147712CAS No.: 2636771-29-2PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature.
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Chelerythrine hydroxide
0 ImagesChelerythrine hydroxide is an alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine hydroxide inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM. Chelerythrine hydroxide triggers Apoptosis and Autophagy. Chelerythrine hydroxide has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine hydroxide shows antibacterial activities against Gram-positive bacteria, Staphylococcus aureus (SA), MRSA.
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MRS2768
0 ImagesCat. No.: HY-108649CAS No.: 1047980-83-5MRS2768 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.
![[Ala107]MBP(104-118) acetate](https://file.medchemexpress.com/product_pic/hy-p1289d.gif "Click to View [Ala107]MBP(104-118) acetate Product Detail")
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Calphostin I
0 ImagesCat. No.: HY-N19701CAS No.: 124857-59-6Calphostin I is a selective protein kinase C (PKC) inhibitor with an IC50 of 0.14 μM in rats. Calphostin I interacts with the regulatory domain of PKC, and the aromatic groups at its C-14 and C-17 positions contribute to enhanced potency and selectivity, with no inhibition of cyclic adenosine monophosphate-dependent protein kinase (PKA) at high concentrations. Calphostin I can be used in research related to cervical cancer and breast cancer.
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[Ala113]MBP(104-118)
![[Ala113]MBP(104-118)](https://file.medchemexpress.com/product_pic/hy-p1289.gif "Click to View [Ala113]MBP(104-118) Product Detail")
0 ImagesCat. No.: HY-P1289CAS No.: 99026-78-5[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.
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HA-100 hydrochloride
0 ImagesCat. No.: HY-100984ACAS No.: 141543-63-7
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[Ala107]MBP(104-118)
![[Ala107]MBP(104-118)](https://file.medchemexpress.com/product_pic/hy-p1289a.gif "Click to View [Ala107]MBP(104-118) Product Detail")
0 ImagesCat. No.: HY-P1289ACAS No.: 99026-77-4[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.
