HCCA2 Inhibitors
HCCA2 inhibitors are a class of chemical compounds that interact specifically with the hydroxycarboxylic acid receptor 2 (HCA2), also known as GPR109A, which is a G protein-coupled receptor (GPCR). The primary endogenous ligands for this receptor are the ketone body β-hydroxybutyrate and the short-chain fatty acids (SCFAs) such as acetic acid and butyric acid. These inhibitors are designed to selectively bind to the HCA2 receptor and modulate its activity. The precise mechanism by which HCCA2 inhibitors exert their effects involves blocking the binding of endogenous ligands to HCA2, thus inhibiting the receptor's normal function. These compounds are structurally diverse, with the key feature being their ability to interact with the active site of the HCA2 receptor and alter its conformation in a way that prevents ligand-induced signaling.
The development of HCCA2 inhibitors is grounded in the intricate understanding of the structure and function of the HCA2 receptor. This GPCR is part of a larger family of receptors that play important roles in various physiological processes by sensing molecules like fatty acids and ketones. HCCA2 inhibitors are characterized by their chemical structure, which allows them to have a high affinity for the HCA2 receptor, and their selectivity, which minimizes interactions with other receptors, thereby reducing off-target effects. The design of these inhibitors often involves a detailed analysis of the receptor-inhibitor interactions, possibly through computational methods like molecular docking and structure-activity relationship (SAR) studies. These research tools help in refining the molecular structure of HCCA2 inhibitors to enhance their potency and selectivity for the HCA2 receptor. The fine-tuning of their chemical properties is crucial for their ability to modulate the receptor's activity in the specific manner intended by their design.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. EGFR signaling can upregulate HCCA2 expression. Thus, by inhibiting EGFR, Erlotinib indirectly decreases HCCA2 expression and activity. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin is an mTOR inhibitor. mTOR signaling is involved in the translational control of a number of proteins, including HCCA2. By inhibiting mTOR, Rapamycin reduces the translation and subsequent activity of HCCA2. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $57.00 $100.00 $250.00 | 129 | |
Sorafenib is a multikinase inhibitor that targets Raf kinases, among others. As Raf is part of the MAPK/ERK pathway, which can regulate HCCA2 expression, Sorafenib can thus decrease HCCA2 activity by inhibiting this pathway. | ||||||
Trametinib | 871700-17-3 | sc-364639 sc-364639A sc-364639B | 5 mg 10 mg 1 g | $114.00 $166.00 $947.00 | 19 | |
Trametinib is a MEK inhibitor. MEK is upstream in the MAPK/ERK pathway, which is known to control the expression and activity of several proteins including HCCA2. Inhibition of MEK by Trametinib can lead to downregulation of HCCA2 activity. | ||||||
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 another EGFR inhibitor that blocks EGFR tyrosine kinase activity. This action potentially reduces signaling through pathways that increase HCCA2 expression, thereby decreasing its activity. | ||||||
Everolimus | 159351-69-6 | sc-218452 sc-218452A | 5 mg 50 mg | $131.00 $651.00 | 7 | |
Everolimus is also an mTOR inhibitor. It works by blocking the activity of mTOR, which is involved in protein synthesis regulation. As a result, HCCA2 synthesis and activity are decreased. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $70.00 $145.00 | 51 | |
Dasatinib is a Src family kinase inhibitor. Src kinases can regulate multiple pathways, potentially affecting HCCA2 signaling. By inhibiting Src kinases, Dasatinib may reduce HCCA2 activity. | ||||||
Sunitinib, Free Base | 557795-19-4 | sc-396319 sc-396319A | 500 mg 5 g | $153.00 $938.00 | 5 | |
Sunitinib is a receptor tyrosine kinase inhibitor. By inhibiting various receptor tyrosine kinases, Sunitinib can affect signaling pathways that modulate HCCA2 activity, leading to its decreased function. | ||||||
Pazopanib | 444731-52-6 | sc-396318 sc-396318A | 25 mg 50 mg | $130.00 $182.00 | 2 | |
Pazopanib inhibits multiple receptor tyrosine kinases. It can diminish signaling through pathways that are known to control HCCA2 expression and activity, leading to a decrease in its activity. | ||||||
Vandetanib | 443913-73-3 | sc-220364 sc-220364A | 5 mg 50 mg | $167.00 $1353.00 | ||
Vandetanib is a tyrosine kinase inhibitor that targets EGFR, VEGFR, and RET. By blocking these receptors, it can impact pathways that regulate HCCA2 expression, reducing HCCA2 activity. | ||||||