ABC1 Inhibitors
ABC1 inhibitors, belonging to the class of organic compounds, are a group of chemical substances characterized by their ability to selectively modulate the activity of ATP-binding cassette sub-family A member 1 (ABC1) protein. This class of inhibitors operates by targeting and binding to the active site or allosteric regions of the ABC1 protein, resulting in the inhibition of its enzymatic or transport function. ABC1, a crucial integral membrane protein, plays a vital role in cellular processes such as lipid transport, maintenance of cellular lipid homeostasis, and cholesterol efflux from cells. As a consequence, ABC1 inhibitors have garnered significant attention due to their potential implications in regulating cellular lipid metabolism and influencing lipid-related diseases.
Structurally diverse, ABC1 inhibitors often possess hydrophobic and polar functional groups, enabling them to interact with specific residues within the active site or regulatory regions of the ABC1 protein. This interaction disrupts the natural conformational changes required for the protein's normal functioning, leading to the modulation of lipid transport and cellular cholesterol levels. Researchers have extensively studied the mechanisms of action of ABC1 inhibitors, uncovering various binding modes and interactions that contribute to their inhibitory effects. The development of these inhibitors involves structure-activity relationship studies, computational modeling, and high-throughput screening techniques to optimize their potency, selectivity, and pharmacokinetic properties. Given the pivotal role of ABC1 in lipid metabolism and related cellular processes, the identification and study of ABC1 inhibitors provide valuable insights into the underlying molecular mechanisms. These inhibitors serve as essential tools in deciphering the complex interplay between lipid homeostasis and disease development, shedding light on potential avenues for future research and drug discovery endeavors aimed at addressing lipid-related disorders.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Imatinib | 152459-95-5 | sc-267106 sc-267106A sc-267106B | 10 mg 100 mg 1 g | $26.00 $119.00 $213.00 | 27 | |
Imatinib is a tyrosine kinase inhibitor that targets BCR-ABL, c-KIT, and PDGFR. It binds to the ATP-binding site of these kinases, inhibiting their activity and thereby blocking downstream signaling pathways responsible for cell proliferation and survival in certain cancers. | ||||||
Gefitinib | 184475-35-2 | sc-202166 sc-202166A sc-202166B sc-202166C | 100 mg 250 mg 1 g 5 g | $63.00 $114.00 $218.00 $349.00 | 74 | |
Gefitinib is an epidermal growth factor receptor (EGFR) inhibitor. It competes with ATP for binding to the EGFR tyrosine kinase domain, preventing activation of downstream signaling pathways that promote cell growth and proliferation. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $57.00 $100.00 $250.00 | 129 | |
Sorafenib inhibits multiple kinases, including RAF kinases and VEGFR. By targeting these kinases, it disrupts cell signaling pathways involved in tumor growth, angiogenesis, and apoptosis. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $70.00 $145.00 | 51 | |
Dasatinib inhibits BCR-ABL, c-KIT, and other tyrosine kinases. It binds to the active site of these kinases, preventing the transfer of phosphate groups and interfering with the growth and survival signals in cancer cells. | ||||||
Lapatinib | 231277-92-2 | sc-353658 | 100 mg | $420.00 | 32 | |
Lapatinib is a dual tyrosine kinase inhibitor of EGFR and HER2. It disrupts downstream signaling pathways involved in cell proliferation and survival, particularly in HER2-positive breast cancer. | ||||||
Erlotinib, Free Base | 183321-74-6 | sc-396113 sc-396113A sc-396113B sc-396113C sc-396113D | 500 mg 1 g 5 g 10 g 100 g | $87.00 $135.00 $293.00 $505.00 $3827.00 | 42 | |
Erlotinib targets EGFR by competing with ATP for binding to the kinase domain. By inhibiting EGFR activity, it interferes with signaling cascades that regulate cell growth and survival. | ||||||
Vemurafenib | 918504-65-1 | sc-364643 sc-364643A | 10 mg 50 mg | $117.00 $423.00 | 11 | |
Vemurafenib targets mutant BRAFV600E kinase, a key player in the MAPK signaling pathway. By inhibiting this kinase, it interferes with abnormal cell proliferation and survival seen in melanomas harboring the specific mutation. | ||||||
Ibrutinib | 936563-96-1 | sc-483194 | 10 mg | $156.00 | 5 | |
Ibrutinib irreversibly inhibits Bruton's tyrosine kinase (BTK), which is essential for B-cell signaling. By blocking BTK activity, it disrupts B-cell receptor signaling, leading to decreased proliferation and increased apoptosis in B-cell malignancies. | ||||||
Ruxolitinib | 941678-49-5 | sc-364729 sc-364729A sc-364729A-CW | 5 mg 25 mg 25 mg | $251.00 $500.00 $547.00 | 16 | |
Ruxolitinib inhibits JAK1 and JAK2, which play a role in cytokine signaling. By blocking these kinases, it interferes with the dysregulated signaling in certain myeloproliferative neoplasms, leading to reduced cell proliferation and inflammation. | ||||||
Abemaciclib | 1231929-97-7 | sc-507342 | 10 mg | $110.00 | ||
Abemaciclib is another CDK 4/6 inhibitor. Like Palbociclib, it blocks the G1-to-S cell cycle transition by inhibiting CDK4/6 and retinoblastoma protein phosphorylation, thereby potentially limiting cell cycle progression and proliferation in specific cancers. | ||||||