Date published: 2025-10-15

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H2-Aa Inhibitors

Chemical inhibitors of H2-Aa play a significant role in modulating the antigen presentation process by affecting different aspects of the intracellular environment necessary for H2-Aa function. Chloroquine, Bafilomycin A1, Concanamycin A, and NH4Cl are all agents that disrupt the acidic pH within endosomes, which is crucial for the optimal activity of H2-Aa. Chloroquine functions by inhibiting endosomal acidification, thereby potentially altering the antigen processing that H2-Aa mediates. Similarly, Bafilomycin A1 and Concanamycin A, as vacuolar-type H+-ATPase inhibitors, prevent the acidification of vesicles, which is a prerequisite for the proper operation of H2-Aa. NH4Cl, on the other hand, raises the pH in acidic compartments through the diffusion of ammonia, leading to a functional impairment of H2-Aa due to the disrupted pH gradient.

On the other end of the spectrum, Monensin, an ionophore, exchanges H+ and Na+ across the membrane, neutralizing lysosomal pH and, therefore, affecting the antigen processing role of H2-Aa. Protease inhibitors such as Leupeptin, E64, and Pepstatin A target different proteolytic enzymes that are integral to the antigen processing pathway. Leupeptin inhibits cysteine and serine proteases, while E64 specifically inhibits cysteine proteases, and Pepstatin A targets aspartic proteases, all of which are essential for the generation of peptides that H2-Aa presents. Furthermore, proteasome inhibitors Lactacystin and MG132 obstruct the degradation of cytosolic proteins into peptides. By blocking this step, these inhibitors directly impede the supply of peptides necessary for the function of H2-Aa, thereby inhibiting its role in antigen presentation.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Chloroquine

54-05-7sc-507304
250 mg
$68.00
2
(0)

Chloroquine is an antimalarial agent that can inhibit the endosomal acidification. H2-Aa is involved in antigen processing within endosomes. Inhibition of endosomal acidification by Chloroquine could, therefore, prevent proper antigen processing, leading to a functional inhibition of H2-Aa in its role of antigen presentation.

Bafilomycin A1

88899-55-2sc-201550
sc-201550A
sc-201550B
sc-201550C
100 µg
1 mg
5 mg
10 mg
$96.00
$250.00
$750.00
$1428.00
280
(6)

Bafilomycin A1 is a specific inhibitor of the vacuolar-type H+-ATPase. By inhibiting this ATPase, the acidification of endosomes is prevented. Since H2-Aa requires the acidic environment of endosomes for proper antigen processing and presentation, Bafilomycin A1 can functionally inhibit H2-Aa by disrupting this environment.

Concanamycin A

80890-47-7sc-202111
sc-202111A
sc-202111B
sc-202111C
50 µg
200 µg
1 mg
5 mg
$65.00
$162.00
$650.00
$2550.00
109
(2)

Concanamycin A is also an inhibitor of the vacuolar-type H+-ATPase like Bafilomycin A1. It inhibits the acidification of intracellular compartments, which is essential for the function of H2-Aa in antigen processing. Therefore, Concanamycin A can functionally inhibit H2-Aa by preventing the acidification required for its function.

Monensin A

17090-79-8sc-362032
sc-362032A
5 mg
25 mg
$152.00
$515.00
(1)

Monensin is an ionophore that disrupts lysosomal pH through the exchange of H+ and Na+ across membranes. This ion exchange can neutralize the acidic environment necessary for the function of H2-Aa in antigen processing. Thus, Monensin functionally inhibits H2-Aa by disrupting the pH gradient needed for its activity.

Ammonium Chloride

12125-02-9sc-202936
sc-202936A
sc-202936B
25 g
500 g
2.5 kg
$38.00
$54.00
$147.00
4
(1)

Ammonium chloride (NH4Cl) raises the pH in acidic intracellular compartments such as endosomes. Since H2-Aa requires an acidic environment for optimal antigen processing, NH4Cl can functionally inhibit H2-Aa by alkalinizing the endosomal pH and interfering with its normal function of antigen presentation.

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
$72.00
$145.00
$265.00
$489.00
$1399.00
$99.00
19
(3)

Leupeptin is a protease inhibitor that can block the activity of several cysteine and serine proteases within the endosomes/lysosomes. By inhibiting these proteases, Leupeptin can affect the processing of antigens that H2-Aa presents, thereby functionally inhibiting H2-Aa by preventing the presentation of properly processed antigens.

E-64

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

E64 is another protease inhibitor that specifically inhibits cysteine proteases. The inhibition of these enzymes disrupts the breakdown of proteins into peptides that are essential for binding to H2-Aa. Hence, E64 can functionally inhibit H2-Aa by preventing antigen processing necessary for H2-Aa to present peptides.

Lactacystin

133343-34-7sc-3575
sc-3575A
200 µg
1 mg
$165.00
$575.00
60
(2)

Lactacystin is a proteasome inhibitor that prevents the degradation of cytosolic proteins into peptides. These peptides are necessary for the function of H2-Aa in antigen presentation. Thus, Lactacystin can functionally inhibit H2-Aa by blocking the supply of peptides necessary for presentation.

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)

MG132 is another proteasome inhibitor that blocks the degradation of proteins into peptides. By inhibiting the proteasome, MG132 prevents the generation of peptides that bind to H2-Aa for antigen presentation. Therefore, MG132 can functionally inhibit H2-Aa by precluding the peptide generation it requires.