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]
-
PKCα Related Products (46)
-
Antibodies (2)
-
Midostaurin
0 ImagesSynonyms: PKC412; CGP 41251Midostaurin (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.
-
Rottlerin
0 ImagesRottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.
-
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.
-
Darovasertib
0 ImagesSynonyms: LXS196; IDE196
-
CMPD101
0 ImagesCMPD101 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.
-
Ruboxistaurin
0 ImagesSynonyms: LY333531
-
Ro 31-8220 mesylate
0 ImagesSynonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylateRo 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.
-
(-)-Indolactam V
0 ImagesSynonyms: Indolactam V(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
-
Ruboxistaurin hydrochloride
0 ImagesSynonyms: LY333531 hydrochloride
-
PKCβ inhibitor 1
0 ImagesPKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
-
Bisindolylmaleimide I hydrochloride
0 ImagesSynonyms: GF109203X hydrochloride; Go 6850 hydrochloride
-
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.
