PKCα
PKCα is a widely expressed AGC-family serine/threonine kinase that regulates proliferation, apoptosis, differentiation, motility, and inflammation[1]. Mechanistically, PKCα links lipid-dependent PKC signaling to tissue-specific outputs, so its activation or overexpression can produce cell growth, cell-cycle arrest, or differentiation depending on cellular context[1]. In disease models, PKCα regulates cardiac contractility, atherogenesis, cancer, and arterial thrombosis, and Prkca-deficient mouse hearts show hypercontractility through altered Ca2+ handling[2][3]. Compared with related isoforms, PKCα shares lipid-dependent PKC activation logic but differs from PKCδ in structural features, activation requirements, and sometimes opposing biological functions[4]. For experimental applications, GF109203X provides a potent PKC inhibitor tool, while AEB071/sotrastaurin inhibits classical and novel PKC isotypes and blocks early T-cell activation[5][6].
References:
- [1]. Nakashima S. Protein kinase C alpha (PKC alpha): regulation and biological function. J Biochem. 2002 Nov;132(5):669-75. doi: 10.1093/oxfordjournals.jbchem.a003272. PMID: 12417014. et al. Protein kinase C alpha (PKC alpha): regulation and biological function. J Biochem. 2002 Nov;132(5):669-75. [Content Brief]
- [2]. Konopatskaya O, et al. Protein kinase Calpha: disease regulator and therapeutic target. Trends Pharmacol Sci. 2010 Jan;31(1):8-14. [Content Brief]
- [3]. Braz JC, et al. PKC-alpha regulates cardiac contractility and propensity toward heart failure. Nat Med. 2004 Mar;10(3):248-54. [Content Brief]
- [4]. Black JD, et al. PKCα and PKCδ: Friends and Rivals. J Biol Chem. 2022 Aug;298(8):102194. [Content Brief]
- [5]. Toullec D, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C[J]. Journal of biological chemistry, 1991, 266(24): 15771-15781.
- [6]. Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330(3):792-801. [Content Brief]
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PKCα Related Products (48)
Related Products (48)
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Antibodies (2)
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Bisindolylmaleimide VIII acetate
0 ImagesSynonyms: Ro 31-7549 acetate; Bis VIII acetateBisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
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PKC-theta inhibitor 1
0 ImagesPKC-theta inhibitor 1 is an orally active and selective ATP-competitive inhibitor of Protein Kinase Cθ (PKCθ), with a Ki value of 6 nM. PKC-theta inhibitor 1 inhibits T-cell-mediated inflammatory responses by suppressing the release of proinflammatory cytokines (IL-2 IC50 = 0.21 μM in anti-CD3/CD28-stimulated PBMCs; IL-17 IC50 = 1 μM in CD3/CD28-stimulated Th17 cells) PKC-theta inhibitor 1 significantly reduces symptoms in mice with ongoing experimental autoimmune encephalomyelitis (EAE). PKC-theta inhibitor 1 can be used for the study of T-cell-mediated inflammatory diseases such as multiple sclerosis.
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PKC-IN-6
0 ImagesPKC-IN-6 is a selective inhibitor of protein kinase C-α (PKC-α) with an IC50 of 240 μM. PKC-IN-6 shows no inhibitory activity against PKC-δ, PKA or EGF-R tyrosine kinase. PKC-IN-6 can be used in research related to bladder cancer.
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Reproxalap
0 ImagesSynonyms: ADX-102; NS-2Reproxalap (ADX-102) is an active aldehyde sequestering agent. Reproxalap reduces the PKCα activity. Reproxalap blocks caspase 3/7 activation. Reproxalap protects cells from the cytotoxicity of C18:0-al. Reproxalap has anti-inflammatory and pain-relieving effects. Reproxalap is used in studies of dry eye, allergic conjunctivitis, and non-infectious anterior uveitis.
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Ro 31-8220 formic
0 ImagesCat. No.: HY-13866BPurity: 99.76%Synonyms: Bisindolylmaleimide IX formicRo 31-8220 formic 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 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Ro 31-8220 formic 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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PKCiota-IN-2 formic
0 ImagesCat. No.: HY-122858APurity: 99.04%PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
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Bisindolylmaleimide III
0 ImagesBisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer.
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Bisindolylmaleimide XI hydrochloride
0 ImagesSynonyms: Ro 32-0432; Ro 31-8830 hydrochloride
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Ruboxistaurin mesylate
0 ImagesSynonyms: LY333531 mesylateRuboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.
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(S)-Ro 32-0432
0 ImagesCat. No.: HY-108601ACAS No.: 1781828-85-0(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
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βGlcCer
0 ImagesCat. No.: HY-152940CAS No.: 887907-50-8Synonyms: C24:1 β-glucosylceramideβGlcCer is a glycosphingolipid. βGlcCer directly increases the development and PKCα and PKCδ activation in mouse bone marrow-derived DCs (BMDCs). β-GlcCer accumulating in Gaucher disease activates microglia through macrophage-inducible C-type lectin (Mincle) to induce phagocytosis of living neurons, which exacerbates Gaucher symptoms.
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Ro 31-8220
0 ImagesCat. No.: HY-13866ACAS No.: 125314-64-9Synonyms: Bisindolylmaleimide IXRo 31-8220 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 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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PKCiota-IN-2
0 ImagesCat. No.: HY-122858CAS No.: 2230055-52-2PKCiota-IN-2 (Compound 49) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
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PF-04577806
0 ImagesCat. No.: HY-139467CAS No.: 1072100-81-2
