gp91phox Inhibitors
Chemical inhibitors of gp91phox target various aspects of the enzyme's function to impede its role in producing reactive oxygen species (ROS). Diphenyleneiodonium chloride acts on gp91phox by binding to its flavoprotein domain, essential for catalytic activity, thus blocking electron transfer from NADPH to oxygen. Apocynin interferes with the assembly of the NADPH oxidase complex, critical for gp91phox activation, by hindering the interaction between the p47phox and p22phox subunits. AEBSF and its hydrochloride form, 4-(2-Aminoethyl) benzenesulfonyl fluoride, inhibit the proteolytic processing of gp91phox, thereby curbing the enzyme's maturation and function. GKT137831, as a dual inhibitor, selectively targets the NOX1/NOX4 isoforms that include gp91phox within the NOX2 complex, reducing the enzyme's capacity to generate ROS.
VAS2870 and VAS3947, as pan-NADPH oxidase inhibitors, non-competitively inhibit electron transfer within the NOX enzyme complex, a crucial step for ROS generation by gp91phox. ML171, though specifically an inhibitor of the NOX1 isoform, can indirectly diminish gp91phox activity by targeting a related mechanism. GLX351322, primarily an inhibitor of NOX4, also exhibits a suppressive effect on gp91phox by obstructing electron transfer. Fulvene-5 modifies essential thiol groups of gp91phox, leading to inhibition of its ROS production. Plumbagin utilizes redox cycling to interfere with electron transfer processes within the NADPH oxidase complex, thereby reducing gp91phox activity. Lastly, Ebselen acts by mimicking glutathione peroxidase activity, interacting with peroxides to lower ROS levels produced by gp91phox. Each inhibitor employs a distinct method to inhibit the enzymatic activity of gp91phox, demonstrating the complexity of regulating this enzyme's function.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Diphenyleneiodonium chloride | 4673-26-1 | sc-202584E sc-202584 sc-202584D sc-202584A sc-202584B sc-202584C | 10 mg 25 mg 50 mg 100 mg 250 mg 500 mg | $148.00 $133.00 $311.00 $397.00 $925.00 $1801.00 | 24 | |
Diphenyleneiodonium chloride (DPI) inhibits gp91phox by binding to the flavoprotein domain of the enzyme, which is necessary for its catalytic activity. DPI acts as a flavoenzyme inhibitor that blocks electron transfer from NADPH to the oxygen molecule, thereby inhibiting the reactive oxygen species (ROS) generation that gp91phox is responsible for in the NADPH oxidase complex. | ||||||
Apocynin | 498-02-2 | sc-203321 sc-203321A sc-203321B sc-203321C | 1 g 10 g 100 g 500 g | $26.00 $67.00 $114.00 $353.00 | 74 | |
Apocynin inhibits gp91phox by preventing the assembly of the NADPH oxidase complex. It does this by interfering with the interaction between p47phox and p22phox subunits, which are necessary for the activation of gp91phox. This disruption of complex assembly effectively inhibits the production of ROS by gp91phox. | ||||||
AEBSF hydrochloride | 30827-99-7 | sc-202041 sc-202041A sc-202041B sc-202041C sc-202041D sc-202041E | 50 mg 100 mg 5 g 10 g 25 g 100 g | $50.00 $120.00 $420.00 $834.00 $1836.00 $4896.00 | 33 | |
AEBSF is an irreversible serine protease inhibitor that can inhibit gp91phox by preventing the proteolytic processing of the protein necessary for its maturation and function. By inhibiting this processing, AEBSF reduces the functional enzyme available for ROS production. | ||||||
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione | sc-501137 | 25 mg | $380.00 | |||
GKT137831 selectively inhibits gp91phox by targeting the NOX1/NOX4 isoforms of NADPH oxidase. It is a dual inhibitor that impairs the activity of gp91phox within the NOX2 complex, leading to a reduction in ROS generation which is a primary function of gp91phox. | ||||||
2-Acetylphenothiazine | 6631-94-3 | sc-223384 sc-223384A | 25 g 100 g | $74.00 $222.00 | ||
ML171, also known as 2-acetylphenothiazine, selectively inhibits gp91phox by targeting the NOX1 isoform of NADPH oxidase. While NOX1 is distinct from gp91phox (NOX2), the inhibitor can indirectly reduce the overall activity of NADPH oxidase by targeting a similar mechanism that is important for the function of gp91phox. | ||||||
Plumbagin | 481-42-5 | sc-253283 sc-253283A | 100 mg 250 mg | $51.00 $61.00 | 6 | |
Plumbagin inhibits gp91phox through redox cycling and by interfering with the electron transfer within the NADPH oxidase complex. This interference reduces the ability of gp91phox to generate ROS, thereby inhibiting its primary function. | ||||||
Ebselen | 60940-34-3 | sc-200740B sc-200740 sc-200740A | 1 mg 25 mg 100 mg | $32.00 $133.00 $449.00 | 5 | |
Ebselen is a seleno-organic compound that inhibits gp91phox by mimicking glutathione peroxidase activity and reacting with peroxides. This leads to a reduction in ROS levels, which are normally produced by the activity of gp91phox, thus functionally inhibiting the protein. | ||||||