Table 2.

Selectivity of commercially available LOX inhibitors for rat 12/15-LOX enzymes

Drug	Target						Conc (μM)	IC50 (μM)	HXB3 inhibition (%)		12-HETE inhibition (%)
	12	12b	12e	e3	15	15b			12	15	12	15
NDGA	++	+	+	−, #	++	+	30	0.20–30.0	80 ± 1***	90 ± 1***	53 ± 2***	85 ± 1***
AA861	++	−	+	+	+	+	10	0.80	38 ± 2**	25 ± 10	61 ± 1***	55 ± 4**
CDC	++	++	++	++	++	++	10	0.06–3.33	86 ± 1***	77 ± 2***	48 ± 5***	71 ± 1***
BAIC	+	++	+	++	++	+	10	0.12–5.00	77 ± 1***	38 ± 7**	11 ± 3	48 ± 7**
PD	+	+	++	++	−	++	10	0.50–0.80	33 ± 5**	8 ± 4	5 ± 6	3 ± 6

LC-MS/MS analysis of HXB₃, 12-HETE, or 15-HETE formation from AA reveals multiple isozyme targets of 5-, 12- and 15-LOX inhibitors. 12, Alox12; 12b, Alox12b; 12e, Alox12e; e3, Aloxe3; 15, Alox15; 15b, Alox15b; conc, concentration. +, significant inhibition of either HXB₃ or 12-HETE; ++, significant inhibition of both HXB₃ and 12-HETE; −, no change;

^#, significant inhibition of eLOX3-mediated production of HXB₃ observed at 100 μM NDGA. n = 4 wells/treatment.

^**P < 0.01,

^***P < 0.001 vs. vehicle (0.1% DMSO) plus AA.