EC Number   |
Inhibitors |
Structure |
|---|
    1.1.1.239 | (2E)-3-(3,3-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)prop-2-enoate |
- |
   |
| 1.1.1.239 | (2E)-3-(4-bromophenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid |
93.3% inhibition at 0.1 mM |
|
| 1.1.1.239 | (2E)-3-(4-ethylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid |
89.1% inhibition at 0.1 mM |
|
| 1.1.1.239 | (2E)-3-(4-methylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid |
92.7% inhibition at 0.1 mM |
|
| 1.1.1.239 | (2E)-3-prop-2-enoic acid |
- |
|
| 1.1.1.239 | (2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate |
- |
|
| 1.1.1.239 | (2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoic acid |
i.e. baccharin, a component of Brazilian propolis, exhibits a high inhibitory potency and selectivity for AKR1C3 over other AKR1C isoforms. When the cinnamic acid group of baccharin is esterified, there is a dramatic decrease in potency and selectivity for AKR1C3 in comparison to baccharin. Low or submicromolar inhibition is observed when the 3-prenyl group of baccharin is removed, and the selectivity over AKR1C2 is low. Inhibition of NAD+ dependent oxidation of S-tetralol |
|
| 1.1.1.239 | (2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate |
- |
|
| 1.1.1.239 | (2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoic acid |
- |
|
| 1.1.1.239 | (2E)-3-[4-(benzoyloxy)phenyl]prop-2-enoic acid |
- |
|
