Target Validation Information
TTD ID	T12808
Target Name	Protein kinase C alpha (PRKCA)
Type of Target	Successful
Drug Potency against Target	Sotrastaurin acetate	Drug Info	Ki = 0.22 nM	[11]
		Drug Info	IC50 = 3 nM	[3]
	(-)-Cercosporamide	Drug Info	IC50 = 1020 nM	[7]
	1,2-dioctanoyl-sn-glycerol	Drug Info	Ki = 40.1 nM	[8]
	3-(1H-Indol-3-yl)-4-phenylamino-pyrrole-2,5-dione	Drug Info	IC50 = 7233 nM	[4]
	Acteoside	Drug Info	IC50 = 9300 nM	[10]
	BALANOL	Drug Info	IC50 = 70 nM
	CALCEOLARIOSIDE A	Drug Info	IC50 = 600 nM	[10]
	CALCEOLARIOSIDE B	Drug Info	IC50 = 4600 nM	[10]
	Diheptan-3-yl 5-(hydroxymethyl)isophthalate	Drug Info	Ki = 319 nM	[8]
	Dihexan-3-yl 5-(hydroxymethyl)isophthalate	Drug Info	Ki = 661 nM	[8]
	FORSYTHIASIDE	Drug Info	IC50 = 1900 nM	[10]
	LEUCOSCEPTOSIDE A	Drug Info	IC50 = 19000 nM	[10]
	LY-317644	Drug Info	IC50 = 6400 nM
	LY-326449	Drug Info	IC50 = 630 nM	[9]
	Plantainoside D	Drug Info	IC50 = 14800 nM	[10]
	PROSTRATIN	Drug Info	Ki = 12.5 nM	[5]
	PUNICAFOLIN	Drug Info	IC50 = 4000 nM
	RO-316233	Drug Info	IC50 = 550 nM	[6]
	Ro-32-0557	Drug Info	IC50 = 2.85 nM
	RO-320432	Drug Info	IC50 = 8.8 nM
	Ro31-8220	Drug Info	IC50 = 33 nM	[2]
	[2,2':5',2'']Terthiophen-4-yl-methanol	Drug Info	IC50 = 3000 nM	[1]
	[2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde	Drug Info	IC50 = 700 nM	[1]
	[2,2':5',2'']Terthiophene-4-carbaldehyde	Drug Info	IC50 = 5000 nM	[1]
Action against Disease Model	Sotrastaurin acetate	Drug Info	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.
References
REF 1	Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.
REF 2	Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
REF 3	Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 4	Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.
REF 5	A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1. J Med Chem. 1992 May 29;35(11):1978-86.
REF 6	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 7	(-)-Cercosporamide derivatives as novel antihyperglycemic agents. Bioorg Med Chem Lett. 2009 Feb 1;19(3):724-6.
REF 8	Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C. J Med Chem. 2009 Jul 9;52(13):3969-81.
REF 9	(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... J Med Chem. 1996 Jul 5;39(14):2664-71.
REF 10	Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity. J Nat Prod. 1998 Nov;61(11):1410-2.
REF 11	Small molecule inhibitors of PKCTheta as potential antiinflammatory therapeutics. Curr Top Med Chem. 2009;9(7):640-54.

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