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 (51)
Related Products (51)
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Antibodies (2)
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PF-04577806
0 ImagesCat. No.: HY-139467CAS No.: 1072100-81-2
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AS2521780
0 ImagesCat. No.: HY-12663CAS No.: 1214726-89-2AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
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Aurora A/PKC-IN-1
0 ImagesCat. No.: HY-144307CAS No.: 3031505-76-4
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(E/Z)-Chk2-IN-1
0 ImagesCat. No.: HY-112477ACAS No.: 693222-51-4Synonyms: (E/Z)-Hymenialdisine analogue-1(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
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Bisindolylmaleimide III hydrochloride
0 ImagesCat. No.: HY-112454CAS No.: 683775-59-9Bisindolylmaleimide III hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride can be used in studies of signal transduction and colorectal cancer.
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PKCiota-IN-1
0 ImagesCat. No.: HY-122857CAS No.: 2230052-97-6PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively.
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CMPD101 hydrochloride
0 ImagesCat. No.: HY-103045ACAS No.: 1941168-71-3CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively).
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1,2-Dipalmitoyl-sn-glycerol (Standard)
0 ImagesCat. No.: HY-W010736RCAS No.: 30334-71-51,2-Dipalmitoyl-sn-glycerol (Standard) is the analytical standard of 1,2-Dipalmitoyl-sn-glycerol (HY-W010736). This product is intended for research and analytical applications. 1,2-Dipalmitoyl-sn-glycerol is a diacylglycerol that activates PKC. 1,2-Dipalmitoyl-sn-glycerol promotes GLUT4 translocation to the cell surface and recruitment to the plasma membrane of adipocytes. 1,2-Dipalmitoyl-sn-glycerol can be used in research on type 2 diabetes.
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Bisindolylmaleimide VIII
0 ImagesCat. No.: HY-129624CAS No.: 125313-65-7Synonyms: Ro 31-7549; Bis VIIIBisindolylmaleimide 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-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
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Balanol
0 ImagesCat. No.: HY-121197CAS No.: 63590-19-2Synonyms: Ophiocordin; AzepinostatinBalanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides.
