Target Validation Information
TTD ID	T40276
Target Name	Protein kinase C beta (PRKCB)
Type of Target	Clinical trial
Drug Potency against Target	Enzastaurin	Drug Info	IC50 = 30 nM	[10]
	Sotrastaurin acetate	Drug Info	Ki = 0.64 nM	[9]
		Drug Info	IC50 = 3 nM	[2]
	(-)-Cercosporamide	Drug Info	IC50 = 350 nM	[6]
	3-(1H-Indol-3-yl)-4-phenylamino-pyrrole-2,5-dione	Drug Info	IC50 = 223 nM	[3]
	BALANOL	Drug Info	IC50 = 40 nM
	LY-317644	Drug Info	IC50 = 6400 nM
	LY-326449	Drug Info	IC50 = 630 nM	[7]
	PROSTRATIN	Drug Info	Ki = 12.5 nM	[4]
	PUNICAFOLIN	Drug Info	IC50 = 4000 nM
	RO-316233	Drug Info	IC50 = 550 nM	[5]
	Ro-32-0557	Drug Info	IC50 = 6.8 nM
	RO-320432	Drug Info	IC50 = 30.5 nM
	[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	Enzastaurin	Drug Info	Enzastaurin (LY317615.HCl) is an antiproliferative agent targeted specifically against PKC-|?? We have investigated the antit uMoral effects of Enzastaurin against h uMan cancercell lines (NSCLC, colon, and thyroid) and freshly explanted h uMan t uMor tissue. Inhibition of cell growth was observed for lung, colorectal, and thyroid cancer cell lines in a concentration dependent manner. Patient specimens exposed 1 h or 21 days to 1,400 nM Enzastaurin demonstrated inhibition rates of 24 and 32%, respectively. Marked inhibitory effects were observed in breast, thyroid, head/neck, non-small cell lung cancer, pancreatic cancer, and melanoma. In addition to its established antiangiogenic effects, Enzastaurin has direct antit uMor activity against established h uMan cancer cell lines and primary t uMor specimens. IC50 values of Enzastaurin (nM) for established non-small cell lung, colon, and thyroid cancer cell lines Calu1 3,600 Calu3 90 Calu6 4,050 NCI-H520 1,150, HCT-116 8,800, B-CPAP 12	[8]
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	Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 3	Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.
REF 4	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 5	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 6	(-)-Cercosporamide derivatives as novel antihyperglycemic agents. Bioorg Med Chem Lett. 2009 Feb 1;19(3):724-6.
REF 7	(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 8	Antitumor activity of enzastaurin (LY317615.HCl) against human cancer cell lines and freshly explanted tumors investigated in in-vitro [corrected] ... Invest New Drugs. 2007 Jun;25(3):205-10.
REF 9	The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J Clin Invest. 2008 Sep;118(9):3151-9.
REF 10	Small molecule inhibitors of PKCTheta as potential antiinflammatory therapeutics. Curr Top Med Chem. 2009;9(7):640-54.

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