Date published: 2025-10-15

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HtrA2 Inhibitors

HtrA inhibitors encompass a diverse array of chemical entities that intercede in the proteolytic activity of the HtrA family of serine proteases. These compounds operate by either directly interacting with the active site of the enzyme or altering the substrate accessibility. For instance, Ucf-101 functions by binding to the protease domain of HtrA1, thereby preventing its enzymatic activity. Other inhibitors such as Doxycycline, while not selective, have been shown to exert an indirect effect on protein synthesis, which can lead to a reduction in the load of misfolded proteins, indirectly mitigating the cellular demand for HtrA protease activity. Furthermore, compounds like MG-132 interpose the ubiquitin-proteasome pathway, leading to the accumulation of proteins that would otherwise be degraded, thus potentially reducing the need for HtrA activity. Several of these inhibitors are not exclusive to HtrA proteins and possess broad-spectrum activity across various proteases, impacting proteolytic pathways and protein homeostasis in the cell. This includes agents such as Gabexate mesilate and Chymostatin, which are known to inhibit a range of serine proteases. These compounds, through their broad mechanism of action, can affect the proteolytic balance within the cell, hence indirectly modulating the functional activity of HtrA proteins. While the diversity of these chemicals spans different origins and structures, from synthetic compounds like PD150606 to naturally occurring catechins like EGCG, they all share the commonality of interfacing with protease activity within the cellular milieu, thereby holding the potential to modulate the functional dynamics of HtrA serine proteases.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Omi/HtrA2 Protease Inhibitor, Ucf-101

313649-08-0sc-222101
10 mg
$200.00
1
(1)

Ucf-101, an Omi/HtrA2 protease inhibitor, selectively binds to the active site of the HtrA2 protein, disrupting its proteolytic activity. This interaction alters the conformational dynamics of HtrA2, influencing its role in mitochondrial stress responses. The compound exhibits unique reaction kinetics, characterized by a rapid association and slower dissociation, which enhances its inhibitory effect. Its hydrophobic regions facilitate membrane interactions, impacting cellular localization and function.

Doxycycline-d6

564-25-0 unlabeledsc-218274
1 mg
$16500.00
(0)

Tetracycline antibiotic; binds to the 30S ribosomal subunit, inhibiting protein synthesis. HtrA proteins are involved in protein quality control, and their inhibition can occur indirectly by reducing the overall burden of misfolded proteins.

E-64

66701-25-5sc-201276
sc-201276A
sc-201276B
5 mg
25 mg
250 mg
$275.00
$928.00
$1543.00
14
(0)

A cell-permeable, irreversible inhibitor of cysteine proteases; could reduce the burden on HtrA proteases by limiting substrate availability.

Gabexate mesylate

56974-61-9sc-215066
5 mg
$100.00
(0)

Serine protease inhibitor; while primarily targeting other proteases, it can indirectly reduce proteolytic stress on cellular mechanisms where HtrA is involved.

Chymostatin

9076-44-2sc-202541
sc-202541A
sc-202541B
sc-202541C
sc-202541D
5 mg
10 mg
25 mg
50 mg
100 mg
$153.00
$255.00
$627.00
$1163.00
$2225.00
3
(1)

Inhibitor of chymotrypsin-like proteases; can also decrease the overall protease load and indirectly reduce HtrA activity by reducing protein misfolding and aggregation.

PD 151746

179461-52-0sc-222134
5 mg
$192.00
3
(1)

Calpain inhibitor; indirectly affects protease pathways and could reduce the proteolytic processing within cells, possibly affecting HtrA activity.

MG-132 [Z-Leu- Leu-Leu-CHO]

133407-82-6sc-201270
sc-201270A
sc-201270B
5 mg
25 mg
100 mg
$56.00
$260.00
$980.00
163
(3)

A proteasome inhibitor; by blocking proteasomal degradation, it could lead to a reduced need for HtrA activity as misfolded proteins accumulate.

(−)-Epigallocatechin Gallate

989-51-5sc-200802
sc-200802A
sc-200802B
sc-200802C
sc-200802D
sc-200802E
10 mg
50 mg
100 mg
500 mg
1 g
10 g
$42.00
$72.00
$124.00
$238.00
$520.00
$1234.00
11
(1)

A catechin found in green tea; known to modulate various signaling pathways and protease activities, potentially impacting HtrA function indirectly.

Pioglitazone

111025-46-8sc-202289
sc-202289A
1 mg
5 mg
$54.00
$123.00
13
(1)

PPARγ agonist; alters gene expression and may influence proteostasis, thereby indirectly affecting HtrA function.