Table 1.

Induction of QR1, and Inhibition of NF-κB, iNOS and QR2

	QR1		NF-κB-luciferase		Nitrite assay		QR2
Compd	IRa,b	CDc,d (μM)	Lucif. act. % inhibb,e	IC50f (μM)	% Max Inhibb,g	IC50f (μM)	% Max Inhib	IC50f,h (μM)
1	0.7		50.0 ± 0.7	73.0 ± 0.0	31.5 ± 2.5		N/Ah	N/A
6	1.4		0		2.4 ± 1.1		88.6 ± 1.7	31.1 ± 1.7
8	2.8	27.0	17.5 ± 4.9		70.9 ± 1.1	4.2 ± 0.5	N/A	N/A
9	2.5	29.4	0		44.7 ± 2.2		94.9 ± 1.1	0.186 ± 0.03
10	1.8		0		24.7 ± 4.0		88.7 ± 7.5	18.5 ± 4.4
11	2.7	4.3	54.0 ± 8.5		47.5 ± 7.7		90.4 ± 2.9	36.8 ± 2.7
12	1.5		75.0 ± 5.2	5.19 ± 2.4	84.7 ± 0.0	31.5 ± 0.0	50.3 ± 2.7	26.9 ± 3.6
14	1.0		0		68.6 ± 5.1	26.5 ± 1.5	88.8 ± 2.24	0.69 ± 0.11
15	0.7		99.8 ± 0.1	5.42 ± 0.4	86.5 ± 0.4	28.4 ± 0.4	N/A	N/A
16	1.6		84.2 ± 2.0j		70.9 ± 0.4	33.7 ± 0.4	93.3 ± 0.64	0.16 ± 0.02
17	1.0		91.5 ± 4.8	4.74 ± 2.35	79.2 ± 3.3	17.4 ± 1.2	61.5 ± 2.3	1.4 ± 0.27
28	2.4	23.0	82.0 ± 5.7	9.15 ± 3.18	49.1 ± 1.8		90.2 ± 2.03	13.5 ± 0.93
29	1.2		0		5.5 ± 1.8		89.9 ± 0.5	0.45 ± 0.02
30	1.9		0		16.4 ± 0.4		42.1 ± 0.78	3.3 ± 0.27
31	0.8		10.5 ± 7.8		38.7 ± 1.8		109.1 ± 9.1	60.8 ± 9.86
32	0.8		16.0 ± 5.7		12.5 ± 4.4		90.0 ± 1.51	15.3 ± 0.76
33	0.8		0		29.4 ± 3.3		80.0 ± 2.47	18.2 ± 1.59
34	1.6		72.5 ± 15.2	13.1 ± 0.7	79.7 ± 3.3	7.2 ± 1.1	85.1 ± 0.4	0.32 ± 0.02
35	1.0		18.5 ± 9.2		5.0 ± 2.6		93.6 ± 9.3	35.5 ± 8.2
38	4.7	11.3	48.5 ± 9.2		53.8 ± 9.9	47.0 ± 1.4	100.5 ± 8.6	11.7 ± 3.17
39	1.2		79.2 ± 5.9	6.64 ± 0.76	8.8 ± 5.9		31.2 ± 2.5	10.5 ± 2.7
40	4.2	9.42	93.4 ± 0.2	16.17 ± 3.5	14.6 ± 9.5		74.4 ± 3.81	4.8 ± 0.95
41	3.1	0.012	77.4 ± 2.0	2.46 ± 0.5	0.0 ± 3.3		N/A	N/A
42	6.6	1.83	67.5 ± 3.5	17 ± 0.85	51.9 ± 2.9	48.9 ± 1.6	42.7 ± 3.6	11.3 ± 1.0
43	1.4		92.4 ± 2.3	1.39 ± 1.7	77.7 ± 5.5	34.5 ± 2.0	82.6 ± 1.12	4.1 ± 0.22
44	2.2	1.85	50.5 ± 3.3		51.2 ± 1.8	47.2 ± 1.2	76.7 ± 1.95	0.48 ± 0.09
46	7.9i,j	0.0047	99.5 ± 9.9	2.1 ± 1.3	98.9 ± 0.4	7.2 ± 1.0	64.4 ± 1.21	3.5 ± 0.28
47	0.6 j	4.39	84.5 ± 6.4	2.48 ± 1.3	98.7 ± 3.7	5.9 ± 0.5	56.1 ± 1.9	11.2 ± 1.2
49	3.2	16.6	77.3 ± 7.9j		3.4 ± 11.4		N/A	N/A
51	1.4		52.0 ± 4.24		0.8 ± 13.6		N/A	N/A
52	1.7		52.5 ± 4.95j		0.0 ± 7.3		N/A	N/A
53	1.8		91.9 ± 2.4	1.93 ± 0.3	81.3 ± 0.4	45.6 ± 2.6	6.2 ± 0.76	2.9 ± 1.54
54		0.23
55		0.26

^aIR, induction ratio.

^bTesting concentration, 50 μM (except for 1, which was tested at 100 μM).

^cCD is the concentration that doubles the activity.

^dCD values were determined for phenazines with induction ratios > 2.

^eNF-κB IC₅₀ calculated when inhibition > 70%.

^fIC₅₀, median inhibitory concentration.

^giNOS IC₅₀ calculated when inhibition > 50%.

^hN/A; not applicable, no inhibition; compounds 1 and 8 react directly with the NRH substrate, so no inhibition data could be obtained.

ⁱTesting concentration, 305 nM.

^jCytotoxic at testing concentration.