Table 1 Activity of new rexinoids in iNOS, RXR and SREBP in vitro assays.

Rexinoid	Structure	MW	Efficacy	Safety
Rexinoid	Structure		iNOS suppression IC₅₀ (nM)	SREBP activation Fold induction vs. Control
Bexarotene		348.5	143 ± 19	2.23 ± 0.5
LG100268		363.5	83 ± 14	3.06 ± 0.7
MSU-41404		320.5	340 ± 25	3.07 ± 0.5
MSU-41566		336.2	239 ± 53	1.12 ± 0.5
MSU-41405		338.4	267 ± 32	1.87 ± 0.3
MSU-41407		338.4	334 ± 17	1.08 ± 0.1
MSU-41406		352.5	252 ± 55	1.67 ± 0.2
MSU-41408		324.4	300 ± 79	2.55 ± 0.7
MSU-41403		381	331 ± 45	2.68 ± 0.2
MSU-41845		369.2	338 ± 31	1.45 ± 0.2
MSU-41583		310	290 ± 61	1.59 ± 0.5
MSU-41567		418.5	271 ± 92	1.58 ± 0.2
MSU-41402		353.5	343 ± 62	1.37 ± 0.3
MSU-41564		354.5	248 ± 60	2.62 ± 0.7
MSU-42185		369.2	128 ± 49	1.65 ± 0.1
MSU-41842		368.2	161 ± 42	2.15 ± 0.7
MSU-41843		380.2	274 ± 33	2.48 ± 1.8
MSU-42012		382.3	141 ± 27	4.6 ± 2.3
MSU-42011		382.5	158 ± 35	1.49 ± 0.6
MSU-41582		368.2	295 ± 54	1.38 ± 0.4
MSU-42165		383.3	172 ± 13	2.46 ± 0.5
MSU-42166		381.2	221 ± 51	1.46 ± 0.2
MSU-41844		378.1	389 ± 53	0.96 ± 0.5
MSU-41565		397.6	366 ± 49	1.59 ± 0.2
MSU-41846		383.2	347 ± 31	1.63 ± 0.3

To measure iNOS suppression, RAW264.7 macrophage-like cells were treated with twofold serial dilutions (0–1000 nM) of rexinoids and stimulated with LPS (1 ng/ml) for 24 h. NO in the media was measured by the Griess assay. IC50 values were calculated, and the average IC50 values (mean ± SE) of three independent experiments are shown. To measure SREBP induction, HepG2 liver cancer cells were treated with 300 nM rexinoids for 8 h, and SREBP mRNA expression was determined by RT-PCR. Values represent mean ± SD of 3 independent experiments.

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