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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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.
