xCT Inhibitors
xCT, a membrane-bound transporter protein, plays a crucial role in cellular redox homeostasis by mediating the uptake of cystine, a precursor of the antioxidant glutathione. Functionally, xCT operates as an antiporter, exchanging extracellular cystine for intracellular glutamate in a 1:1 ratio, which is essential for maintaining cellular redox balance, detoxification of reactive oxygen species (ROS), and protection against oxidative stress-induced damage. Glutathione, synthesized from cystine, serves as a major antioxidant molecule, scavenging ROS and protecting cells from oxidative damage, thereby blocking cellular dysfunction, DNA damage, and apoptosis. Moreover, xCT-mediated cystine uptake also influences various cellular processes such as cell proliferation, migration, and survival, highlighting its significance in maintaining cellular homeostasis and promoting cell viability.
Inhibition of xCT function can be achieved through various mechanisms targeting its transport activity, expression levels, or protein stability. One approach to inhibiting xCT involves the development of small molecule inhibitors or blocking peptides that specifically target its transport function, thereby hindering cystine uptake and subsequent glutathione synthesis. Additionally, strategies aimed at downregulating xCT expression or disrupting its interaction with regulatory proteins can effectively attenuate its activity, leading to impaired redox homeostasis and increased susceptibility to oxidative stress-induced damage. Furthermore, modulation of signaling pathways involved in xCT regulation, such as the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, can indirectly inhibit xCT function by suppressing its expression or activity, further compromising cellular antioxidant defenses and promoting oxidative stress-induced cell death. The elucidation of these mechanisms of xCT inhibition provides insights into strategies for targeting oxidative stress-related diseases and conditions, highlighting the importance of understanding xCT's role in cellular redox homeostasis and antioxidant defense mechanisms.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Sulfasalazine | 599-79-1 | sc-204312 sc-204312A sc-204312B sc-204312C | 1 g 2.5 g 5 g 10 g | $61.00 $77.00 $128.00 $209.00 | 8 | |
Sulfasalazine may inhibit xCT by competing with cystine for transport, reducing cystine uptake, and thereby decreasing intracellular glutathione levels, leading to oxidative stress and cytotoxicity in cancer cells. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $57.00 $100.00 $250.00 | 129 | |
Sorafenib, while primarily a kinase inhibitor, has been suggested to inhibit xCT indirectly by modulating signaling pathways that affect xCT expression, potentially reducing cystine uptake in cancer cells. | ||||||
L-Glutamic Acid | 56-86-0 | sc-394004 sc-394004A | 10 g 100 g | $297.00 $577.00 | ||
Glutamate, as a natural ligand of xCT, can inhibit its function in high concentrations by competitive inhibition, disrupting the cystine/glutamate exchange and affecting cellular redox status. | ||||||
Cisplatin | 15663-27-1 | sc-200896 sc-200896A | 100 mg 500 mg | $138.00 $380.00 | 101 | |
Cisplatin, a chemotherapy drug, may indirectly inhibit xCT by forming DNA adducts that modulate gene expression, potentially leading to decreased xCT expression and altered redox homeostasis in cancer cells. | ||||||
Pemetrexed Disodium | 150399-23-8 | sc-219564 | 10 mg | $136.00 | 5 | |
Pemetrexed could inhibit xCT activity indirectly by disrupting folate metabolism, which is crucial for maintaining cellular redox balance, thus potentially influencing xCT function. | ||||||
L-Buthionine sulfoximine | 83730-53-4 | sc-200824 sc-200824A sc-200824B sc-200824C | 500 mg 1 g 5 g 10 g | $286.00 $442.00 $1532.00 $2975.00 | 26 | |
BSO inhibits the synthesis of glutathione, an end product of xCT function, thereby indirectly decreasing xCT's effectiveness in maintaining cellular redox balance. | ||||||
α-Lipoic Acid | 1077-28-7 | sc-202032 sc-202032A sc-202032B sc-202032C sc-202032D | 5 g 10 g 250 g 500 g 1 kg | $69.00 $122.00 $212.00 $380.00 $716.00 | 3 | |
Alpha-Lipoic Acid may inhibit xCT by modulating cellular redox states and influencing the expression or function of xCT, thereby impacting cystine uptake and glutathione synthesis. | ||||||
N-Acetyl-L-cysteine | 616-91-1 | sc-202232 sc-202232A sc-202232C sc-202232B | 5 g 25 g 1 kg 100 g | $34.00 $74.00 $270.00 $114.00 | 34 | |
NAC, while an antioxidant, may paradoxically inhibit xCT by providing cysteine directly, reducing the cellular demand for cystine uptake through xCT and altering redox homeostasis. | ||||||
Dihydro Artemisinin | 71939-50-9 | sc-211332 | 100 mg | $233.00 | 1 | |
Dihydroartemisinin may inhibit xCT by generating reactive oxygen species and altering cellular redox status, potentially leading to decreased xCT expression or activity. | ||||||
Imatinib | 152459-95-5 | sc-267106 sc-267106A sc-267106B | 10 mg 100 mg 1 g | $26.00 $119.00 $213.00 | 27 | |
Imatinib, primarily a tyrosine kinase inhibitor, could indirectly inhibit xCT by modulating pathways that control xCT expression, potentially impacting cystine uptake and redox balance in cancer cells. | ||||||