EC Number |
Inhibitors |
Structure |
---|
3.4.22.68 | 3-[(4-[[2-([(2R,3R)-3-[benzyl(cyclohexa-1,3-dien-1-ylmethyl)carbamoyl]-3-chlorooxiran-2-yl]carbonyl)-2-(carboxymethyl)hydrazinyl]carbonyl]benzyl)carbamoyl]benzoic acid |
partial inhibition of the enzyme |
|
3.4.22.68 | 3-[(4-[[2-[(2E)-4-[bis(naphthalen-1-ylmethyl)amino]-4-oxobut-2-enoyl]-2-(carboxymethyl)hydrazinyl]carbonyl]benzyl)carbamoyl]benzoic acid |
- |
|
3.4.22.68 | 3-[(4-[[2-[4-[bis(naphthalen-1-ylmethyl)amino]-2,3-dichloro-4-oxobutanoyl]-2-(carboxymethyl)hydrazinyl]carbonyl]benzyl)carbamoyl]benzoic acid |
the chlorohydrin form of JCP-666 may inhibit the target SENP by SN2-like displacement of the chloride by the active site cysteine |
|
3.4.22.68 | 3-[(4-[[2-[4-[bis(naphthalen-1-ylmethyl)amino]-3-chloro-2-hydroxy-4-oxobutanoyl]-2-(carboxymethyl)hydrazinyl]carbonyl]benzyl)carbamoyl]benzoic acid |
i.e. JCP-666 |
|
3.4.22.68 | Gu-HCl |
500 mM reduces cleavage to 60%, 1 M reduces cleavage to 0% |
|
3.4.22.68 | hSUMO-VS |
human SUMO protein modified with a vinyl sulfone reactive group after the C-terminal di-glycine, contains the full length SUMO protein fused to a reactive vinyl sulfone group, an irreversible inhibitor of SENP proteases |
|
3.4.22.68 | more |
there may be a connection between a defect in SUMO-1 conjugation to the PML protein and acute promyelocytic leukemia (ALP). Specific Ulp inhibitors can therefore have therapeutic value for ALP |
|
3.4.22.68 | more |
no inhibitory effects are observed with Triton X100 (1 M), imidazole (300 mM), reduced glutathione (20 mM), maltose (20 mM), glycerol (20% v/v), ethylene glycol (20% v/v), sucrose (20% w/v), ethanol (10% v/v) |
|
3.4.22.68 | more |
inhibitor screening, overview. No inhibition by 3-[(4-[[2-[[(2R,3R)-3-(benzylcarbamoyl)-3-chlorooxiran-2-yl]carbonyl]-2-(carboxymethyl)hydrazinyl]carbonyl]benzyl)carbamoyl]benzoic acid, i.e. JCP-667 |
|
3.4.22.68 | N-ethylmaleimide |
NEM, blocks SENP activity by acting as a general alkylating agent that modifies the active site cysteine in parasite lysates |
|