. 2022 Nov 28;13(12):1911–1915. doi: 10.1021/acsmedchemlett.2c00450

Table 1. PHPT1 Inhibition Kinetics of Ethacrynic Acid and Other Electrophiles (n = 3)^a.

inhibitor	k_inact (s^–1)	K_i (μM)	k_inact/K_i (M^–1 s^–1)
ethacrynic acid	2.67 ± 0.02 × 10^–3	183 ± 43	1.46 ± 0.37 × 10¹
N-ethylmaleimide	7.5 ± 1.6 × 10^–3	209 ± 48	3.1 ± 1.1 × 10¹
iodoacetamide	N. I.	N. I.	N. I.
2-iodo-N-phenylacetamide	N. I.	N. I.	N. I.
methyl p-toluenesulfonate	N. I.	N. I.	N. I.
GSSG	N. I.	N. I.	N. I.
norstitic acid²¹	2.8 ± 0.2 × 10^–2	90 ± 20	3.1 ± 1.0 × 10²

N. I. = No appreciable inhibition after 1 h of incubation with the electrophile (25 μM or higher).

Table 1. PHPT1 Inhibition Kinetics of Ethacrynic Acid and Other Electrophiles (n = 3)a.