Inhibitor structure | Chemical or common name | IC50 recombinant CSE | IC50 recombinant CBS | IC50 recombinant 3-MST | Selectivity | Reference |
---|---|---|---|---|---|---|
Aminoethoxyvinyl glycine (AVG) | 1.0 μM1 | No inhibition up to 1 mM1 | No inhibition at 1 mM2 | CSE >>>CBS | 1Asimakopoulou et al., 2013 | |
2Unpublished observations | ||||||
Propargylglycine (PAG) | 40.0 μM1 | No inhibition up to 10 mM1 | No inhibition at 10 mM5 | CSE>>>CBS | 1Asimakopoulou et al., 2013 | |
42.2 μM2 | No inhibition up to 2 mM4 | 2Corvino et al., 2016 | ||||
200 μM3 | 3Sun et al., 2009 | |||||
1 μM or 26 µM4 | 4Zhou et al., 2013 | |||||
5Unpublished observations | ||||||
β-cyano-alanine (BCA) | 14.0 μM (CSE) | 40% inhibition at 10 mM | 15% inhibition at 10 mM2 | CSE>>CBS | 1Asimakopoulou et al., 2013 | |
2Unpublished observations | ||||||
Aminooxyacetic acid (AOAA) | 1.1 μM1 | 8.5 μM1 | No inhibition at 50 μM4 | CSE>CBS | 1Asimakopoulou et al., 2013 | |
2 μM2 | 2Chao et al., 2016 | |||||
3 μM3 | 3Druzhyna et al., 2016 | |||||
4Unpublished observations | ||||||
D-Penicillamine (D-pen) | 270 μM | 8.5 mM | Not tested | CSE>CBS (effect on 3-MST not known) | Brancaleone et al., 2016 | |
Hydroxylamine | 4.8 μM | 278 μM1 | No inhibition at 50 μM3 | CSE>CBS | 1Asimakopoulou et al., 2013 | |
20, 250, or 400 µM2 | 2Zhou et al., 2013 | |||||
3Unpublished observations | ||||||
Trifluoroalanine | 289 μM | 66 μM | Not tested | CBS>CSE (effect on 3-MST not known) | Asimakopoulou et al., 2013 | |
Benserazide | 16% inhibition at 100 μM1 | 30 μM1 | 50% inhibition at 300 μM1 | CBS > CSE>3-MST | 1Druzhyna et al., 2016 | |
125 μM (IC25) 2 | 2Thorson et al., 2013 | |||||
2,3,4-trihydroxybenzylhydrazine (THBH or Ro 04-5127) | Not tested | 30 μM | Not tested | CBS (effect on CSE or 3-MST not known) | Druzhyna et al., 2016 | |
1,6-dimethyl-pyrimido[5,4-e]-1,2,4-triazine-5,7(1H,6H)-dione(NSC 67078) | 30 µM1 | 12 µM1 | Not tested | CBS>CSE (effect on 3-MST not known) | 1Zhou et al., 2013 | |
1 µM2 | 2Druzhyna et al., 2016 | |||||
NSC11041 | 2.5 µM | 4 µM | Not tested | CSE≥CBS (effect on 3-MST not known) | Zhou et al., 2013 | |
JHU-8555 | 25 µM | 8 - 12 µM | Not tested | CBS≥CSE (effect on 3-MST not known) | Zhou et al., 2013 | |
MBSEW03275 | 200 µM | 15 µM | Not tested | CBS>CSE (effect on 3-MST not known) | Zhou et al., 2013 | |
SP14311008 | 40 µM | 20 µM | Not tested | CBS≥CSE (effect on 3-MST not known) | Zhou et al., 2013 | |
Aurintricarboxynic acid | Not tested | 3 µM2 | Not tested | CBS (effect on CSE or 3-MST not known) | Druzhyna et al., 2016 | |
1,4 Naphtoquinone | Not tested | 35 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
2,4-Dinitrophenol | Not tested | 56 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
Piperine | Not tested | 61 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
Apigenin | Not tested | 83 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
Amiloride | Not tested | 89 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
Fraxetin | Not tested | 134 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2013 | |
MNP2-A6 | Not tested | 83 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2015 | |
MNP2-B7 | Not tested | 87 µM | Not tested | CBS (effect on CSE or 3-MST not known) | Thorson et al., 2015 | |
2-Oxo-N-(prop-2-yn-1-yl) thiazolidine-4-carboxamide(SHIP-2a) | 6.3 μM | Not tested | Not tested | CSE (effect on CSE or 3-MST not known) | Corvino et al., 2016 | |
2-(2-((4-Oxo-3,4-dihydroquinazolin-2-yl)thio)acetamido)thiophene-3-carboxamide (Compound 1 or I3MT-1a) | 25% inhibition at 100 μM | 25% inhibition at 100 μM | 1.7 μM | 3-MST | Hanaoka et al., 2017 | |
2-((2-(2,4-Dihydroxyphenyl)-2-oxoethyl)thio)-5,6-dimethylthieno[2,3-dl]pyrimidin-4(3H)-one | Inconclusive due to technical issues | Inconclusive due to technical issues | 6.3 μM | 3-MST (effect on CSE or CBS not clear) | Hanaoka et al., 2017 | |
(Compound 2 I3MT-2a) | ||||||
(2-4-Hydroxy-6-methylpyrimidin-2-yl-sulfanyl-1-naphthalen-1-yl-ethan-1-one) | No inhibition at 100 μM | No inhibition at 100 μM | 2.7 μM | 3-MST | Hanaoka et al., 2017 | |
(Compound 3 or I3MT-3a) | ||||||
3-(Phenylsulfonamido) benzoic acid | 25% inhibition at 100 μM | Enhancement of activity | 5.7 μM | 3-MST | Hanaoka et al., 2017 | |
(Compound 5 or I3MT-5a) |
a Name communicated by author after the publication.