Date published: 2026-4-1

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Abcg3 Inhibitors

Chemical inhibitors of ATP binding cassette subfamily G member 3 (ABCG3) include a diverse array of compounds that interact with the protein in various ways to impede its function. Cyclosporin A, Elacridar, Valspodar, and Glibenclamide can bind to the ATP-binding sites of ABCG3, which is essential for the protein's ability to hydrolyze ATP – an energy source that drives the transport of substrates across the cell membrane. By binding to these sites, these inhibitors prevent ATP hydrolysis, thereby stopping the transport activity of ABCG3. Zosuquidar and Tariquidar, known for their inhibitory action on P-glycoprotein, can also inhibit ABCG3 by binding to allosteric sites or substrate recognition sites. This binding can alter the conformation of the protein, which in turn can prevent the binding and transport of substrates by ABCG3.

Other chemical inhibitors such as Estrogens and Rifampicin interact with ABCG3 in a way that disrupts its transport function. These chemicals may bind directly to the protein, impairing its ability to interact with its substrates. On a different note, Lansoprazole may decrease the proton gradient necessary for the function of ABCG3, as some ABC transporters rely on this gradient for their activity. Progesterone, similar to its inhibition of P-glycoprotein, may bind to regulatory domains on ABCG3, thereby inhibiting the ATPase activity that is crucial for the transport function of the protein. In contrast, MK-571 may inhibit ABCG3 by competitively binding to the protein's substrate-binding sites, which would prevent ABCG3 from interacting with its natural substrates, thereby inhibiting its function. Verapamil, like its action on P-glycoprotein, may block the drug-binding domain of ABCG3, which could impede the protein's ability to transport its substrates across the cell membrane.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Cyclosporin A

59865-13-3sc-3503
sc-3503-CW
sc-3503A
sc-3503B
sc-3503C
sc-3503D
100 mg
100 mg
500 mg
10 g
25 g
100 g
$63.00
$92.00
$250.00
$485.00
$1035.00
$2141.00
69
(5)

Cyclosporin A is known to inhibit various ABC transporters by interfering with their drug efflux function. Considering ABCG3 is an ABC transporter, Cyclosporin A could inhibit this protein by binding to its drug-binding sites and preventing the efflux of substrates.

Elacridar

143664-11-3sc-207613A
sc-207613
sc-207613B
sc-207613C
sc-207613D
5 mg
10 mg
50 mg
100 mg
1 g
$98.00
$113.00
$411.00
$525.00
$2606.00
19
(1)

Elacridar inhibits P-glycoprotein and breast cancer resistance protein by binding to their ATP-binding sites. Similarly, it may inhibit ABCG3 by targeting the ATP-binding sites, thus preventing ATP hydrolysis and substrate transport.

PSC 833

121584-18-7sc-361298
sc-361298A
sc-361298B
sc-361298C
sc-361298D
1 mg
10 mg
50 mg
100 mg
1 g
$217.00
$738.00
$2572.00
$4338.00
$27422.00
12
(1)

Valspodar is a non-immunosuppressive cyclosporin analog that inhibits P-glycoprotein. It would inhibit ABCG3 by binding competitively to the substrate-binding domains, blocking substrate interaction and transport.

MK-571

115103-85-0sc-201340
sc-201340A
5 mg
25 mg
$109.00
$421.00
8
(2)

MK-571 is a leukotriene receptor antagonist that also inhibits the multidrug resistance-associated protein 1 (MRP1), another ABC transporter. It could inhibit ABCG3 by competitively binding to its substrate-binding sites, thereby inhibiting its function.

Verapamil

52-53-9sc-507373
1 g
$374.00
(0)

Verapamil inhibits P-glycoprotein by blocking its drug-binding domain. It may inhibit ABCG3 by a similar mechanism, interfering with the transporter's substrate binding, thus preventing substrate transport.

Lansoprazole

103577-45-3sc-203101
sc-203101A
500 mg
1 g
$59.00
$176.00
6
(0)

Lansoprazole is a proton pump inhibitor that has been shown to inhibit P-glycoprotein. By extension, it could inhibit ABCG3 by decreasing the proton gradient necessary for the function of some ABC transporters, thereby impacting ABCG3's transporter activity.

Progesterone

57-83-0sc-296138A
sc-296138
sc-296138B
1 g
5 g
50 g
$20.00
$52.00
$298.00
3
(1)

Progesterone has been shown to inhibit P-glycoprotein. This inhibition could extend to ABCG3, where progesterone may bind to regulatory domains on ABCG3, leading to inhibition of its ATPase activity and subsequent transport function.

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$97.00
$328.00
$676.00
$1467.00
6
(1)

Rifampicin is an antibiotic that also inhibits various ABC transporters. Its inhibitory effect on ABCG3 could stem from its ability to bind directly to the protein and impair its substrate transport capabilities.

Glyburide (Glibenclamide)

10238-21-8sc-200982
sc-200982A
sc-200982D
sc-200982B
sc-200982C
1 g
5 g
25 g
100 g
500 g
$46.00
$61.00
$117.00
$173.00
$530.00
36
(1)

Glibenclamide, a sulfonylurea compound, has been shown to inhibit the sulfonylurea receptor, which is part of an ABC transporter. It could inhibit ABCG3 by interfering with its ATP-binding domains, which are essential for ATPase activity and substrate transport.