TABLE 4

Recommended in vitro substrates and inhibitors of other non-P450 phase II enzymes

EnzymeSelective Substrates KmSelective InhibitorRecommended Inhibitor Concentration Range (reported IC50 value)References
µMµM
GSTCDNBaEthacrynic acidb0.1–1 mM [IC50 = 6 (α), 0.3 (µ), 3.3 (π)]Polidoro et al., 1981; Warholm et al., 1983; Ploemen et al., 1990
450 (A1–1)
580 (A2–2)
650 (M1a–1a)
910 (P1–1)
NAT1p-Amino benzoic acid (7.5)Caffeic acid0.1–1 mM (Ki = 479)Kukongviriyapan et al., 2006
NAT2Sulfamethazine (40)Curcumin1–100 (Ki = 15)
CES–Temocapril (CES1) (NA)Digitonin0.1–100 (IC50 = 9.2)Nishimuta et al., 2014
Trandolapril (CES1) (1734)BNPPc0.01–10 (IC50 = 0.1)Fukami et al., 2010
Imidapril (CES1) (4.3)
Mycophenolate mofetil (CES1/2) (225- CES1; 22.3- CES2)Telmisartan0.01–10 (IC50 = 0.5)Fukami et al., 2010
Irinotecan (CES2) (14.4)Loperamide0.01–10 (IC50 = 0.1)
BNPPc0.01–10 (IC50 = 0.1)
  • a CDNB: 1-chloro-2,4-dinitrobenzene, nonn-selectiv.e

  • b Partially selective.

  • c Bis(4-nitrophenyl)phosphate (nonspecific).