Date published: 2026-4-24

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TPPII Inhibitors

Tripeptidyl Peptidase II (TPPII) inhibitors encompass a group of compounds that can impede the enzymatic function of TPPII. These inhibitors typically function by binding to the active site of the enzyme, which is responsible for its protease activity. This binding can be either reversible or irreversible, depending on the nature of the inhibitor and the specific chemical interaction it undergoes with the enzyme. For instance, peptide aldehydes, such as AAF-CMK and MG-132, can form a covalent bond with the catalytic serine of TPPII, leading to irreversible inhibition. These compounds mimic the substrate of TPPII and, by binding to the active site, prevent the natural substrate from being processed. On the other hand, reversible inhibitors, such as leupeptin, operate by temporarily occupying the active site without forming a stable covalent bond, allowing them to dissociate from the enzyme over time. Inhibitors like epoxomicin and E-64 contain reactive groups that target specific amino acid residues within the active site of TPPII. For example, epoxomicin can interact with the active site threonine, while E-64 can target the enzyme's cysteine residue. These interactions disrupt the normal catalytic cycle of TPPII, reducing its proteolytic activity. Inhibitors that are not peptide-based, such as lactacystin, provide additional mechanisms of inhibition, further expanding the chemical diversity of TPPII inhibitors. Each inhibitor's specificity and binding affinity for TPPII can vary, leading to differences in their efficiency and mode of inhibition.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Butabindide oxalate

185213-03-0sc-361130
sc-361130A
10 mg
50 mg
$189.00
$770.00
1
(1)

Butabindide oxalate functions as a TPPII, characterized by its capacity to engage in specific electrostatic interactions with active site residues of target proteins. This engagement can lead to conformational changes that modulate enzymatic activity. Its unique steric properties enhance selectivity in binding, while its solubility profile supports effective diffusion across biological membranes. The compound's reactivity as an acid halide further influences its interaction dynamics, shaping the overall biochemical landscape.

AAF-CMK

184901-82-4sc-205591
sc-205591A
5 mg
25 mg
$94.00
$317.00
1
(1)

AAF-CMK acts as a TPPII, distinguished by its ability to form covalent bonds with serine residues in target enzymes, leading to irreversible inhibition. This compound exhibits a unique reactivity profile as an acid halide, facilitating rapid acylation reactions that alter enzyme functionality. Its hydrophobic characteristics enhance membrane permeability, while specific steric configurations promote selective interactions, ultimately influencing kinetic parameters and reaction pathways in biochemical systems.

Cyclo(-Leu-Pro)

2873-36-1sc-285317B
sc-285317
sc-285317A
sc-285317C
100 mg
250 mg
1 g
5 g
$124.00
$259.00
$756.00
$2227.00
(0)

Functions similarly to peptide aldehydes and can inactivate TPPII by forming a covalent bond with the active site serine.

Leupeptin hemisulfate

103476-89-7sc-295358
sc-295358A
sc-295358D
sc-295358E
sc-295358B
sc-295358C
5 mg
25 mg
50 mg
100 mg
500 mg
10 mg
$73.00
$148.00
$316.00
$499.00
$1427.00
$101.00
19
(3)

Leupeptin is a reversible inhibitor that can bind to the active site of TPPII, hindering its enzymatic function.

Epoxomicin

134381-21-8sc-201298C
sc-201298
sc-201298A
sc-201298B
50 µg
100 µg
250 µg
500 µg
$137.00
$219.00
$449.00
$506.00
19
(2)

While primarily an inhibitor of the proteasome, epoxomicin can also inhibit TPPII due to its reactive epoxide group that can interact with the active site threonine.

Calpeptin

117591-20-5sc-202516
sc-202516A
10 mg
50 mg
$121.00
$456.00
28
(1)

Although a calpain inhibitor, this compound can also inhibit TPPII by obstructing the enzyme's active site.

Lactacystin

133343-34-7sc-3575
sc-3575A
200 µg
1 mg
$188.00
$575.00
60
(2)

Lactacystin is known to inhibit the proteasome, but it can also inhibit TPPII by irreversible binding to its active site threonine.

(R)-MG-132

1211877-36-9sc-351846
sc-351846A
sc-351846B
1 mg
5 mg
25 mg
$63.00
$196.00
$843.00
9
(4)

This tripeptide aldehyde can inhibit TPPII activity by binding to the active site and preventing substrate processing.