Target Validation Information
Target ID T12808
Target Name Protein kinase C, alpha type
Target Type
Clinical Trial
Drug Potency against Target LY-317644 Drug Info IC50 = 6400 nM
LY-326449 Drug Info IC50 = 630 nM [534154]
Plantainoside D Drug Info IC50 = 14800 nM [534763]
FORSYTHIASIDE Drug Info IC50 = 1900 nM [534763]
PUNICAFOLIN Drug Info IC50 = 4000 nM
[2,2':5',2'']Terthiophen-4-yl-methanol Drug Info IC50 = 3000 nM [525575]
1,2-dioctanoyl-sn-glycerol Drug Info Ki = 40.1 nM [530134]
3-(1H-Indol-3-yl)-4-phenylamino-pyrrole-2,5-dione Drug Info IC50 = 7233 nM [527221]
CALCEOLARIOSIDE A Drug Info IC50 = 600 nM [534763]
LEUCOSCEPTOSIDE A Drug Info IC50 = 19000 nM [534763]
ACETOSIDE Drug Info IC50 = 9300 nM [534763]
Diheptan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 319 nM [530134]
Sotrastaurin acetate Drug Info Ki = 0.22 nM [552971]
Indolocarbazole analogue Drug Info IC50 = 3 nM [526234]
[2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde Drug Info IC50 = 700 nM [525575]
[2,2':5',2'']Terthiophene-4-carbaldehyde Drug Info IC50 = 5000 nM [525575]
RO-320432 Drug Info IC50 = 8.8 nM
BISINDOLYLMALEIMIDE IX Drug Info IC50 = 33 nM [525872]
CALCEOLARIOSIDE B Drug Info IC50 = 4600 nM [534763]
RO-316233 Drug Info IC50 = 550 nM [528701]
Ro-32-0557 Drug Info IC50 = 2.85 nM
BALANOL Drug Info IC50 = 70 nM
Dihexan-3-yl 5-(hydroxymethyl)isophthalate Drug Info Ki = 661 nM [530134]
(-)-Cercosporamide Drug Info IC50 = 1020 nM [529887]
PROSTRATIN Drug Info Ki = 12.5 nM [527606]
Action against Disease Model Sotrastaurin acetate Total protein kinase C (PKC) activity and the expression of 9 isoforms were determined in the estrogen receptor (ER) positive MCF-7 h uMan breast cancer cell line, this line transfected to overexpress either PKC-???or erbB2, and in 3 ER negative breast cancer cell lines. Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The Prkca(-/-) mice showed no signs of retinal degeneration up to 12 months of age, but ERG measurements indicated a decelerated increase in the ascending limb of the scotopic (rod-sensitive) b-wave as well as a delayed return to baseline. These results suggest that PKC|? is an important modulator that affects bipolar cell signal transduction and termination. Confocal microscopy of retinal sections showed that PKC|? co-localized with calbindin, which indicates a PKC|? localization in close proximity to the horizontal cell terminals. In addition, the implicit time of the ERG c-alpha originating from the retinal pigment epitheli uM (RPE) and the recovery of photoreceptors from bleaching conditions were substantially faster in the knockout mice than in the wild-type control animals???hese results suggest that PKC|? is a modulator of rod-bipolar cell function by accelerating glutamate-driven signal transduction and termination
References
Ref 534154J Med Chem. 1996 Jul 5;39(14):2664-71.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 525575Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 527221Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 552971Small molecule inhibitors of PKCTheta as potential antiinflammatory therapeutics. Curr Top Med Chem. 2009;9(7):640-54.
Ref 526234Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.Mixed lineage kinase activity of indolocarbazole analogues.
Ref 525575Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.
Ref 525575Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.
Ref 525872Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors.
Ref 534763J Nat Prod. 1998 Nov;61(11):1410-2.Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Ref 528701J Med Chem. 1992 Jan;35(1):177-84.Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides.
Ref 530134J Med Chem. 2009 Jul 9;52(13):3969-81.Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Ref 529887Bioorg Med Chem Lett. 2009 Feb 1;19(3):724-6. Epub 2008 Dec 11.(-)-Cercosporamide derivatives as novel antihyperglycemic agents.
Ref 527606J Med Chem. 1992 May 29;35(11):1978-86.A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.

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