c-Erb-A β-1 Inhibitors
The chemical class of c-Erb-A β-1 inhibitors encompasses a variety of compounds that inhibit the function of the thyroid hormone receptor beta-1 (THRβ1). These inhibitors can directly compete with thyroid hormones for receptor binding or modulate receptor activity, gene expression, and hormone synthesis. Direct inhibitors like NH-3 and tetrac act by occupying the ligand-binding domain of THRβ1, preventing the association of thyroid hormones, which is necessary for receptor activation and downstream gene transcription. Compounds such as 1-850 are designed to selectively antagonize THRβ1, reducing its transcriptional activity.
Some compounds may act as selective modulators, such as GC-1, which can also function as an antagonist under certain circumstances by inhibiting coactivator recruitment to THRβ1. Amiodarone, due to its structural similarity to thyroxine (T4), can interfere with thyroid hormone action, impacting THRβ1 function. Other inhibitors indirectly decrease THRβ1 activation by lowering thyroid hormone levels. MMI and PTU are antithyroid drugs that inhibit the synthesis of thyroid hormones, while ketoconazole affects hormone metabolism. Dexamethasone influences receptor expression, altering THRβ1's transcriptional activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Glutathione, reduced | 70-18-8 | sc-29094 sc-29094A | 10 g 1 kg | $76.00 $2050.00 | 8 | |
Glutathione can form disulfide bonds with cysteine residues in the c-Erb A β1, potentially altering the receptor′s conformation and inhibiting its ability to bind to DNA response elements, which is essential for its function. | ||||||
Methimazole | 60-56-0 | sc-205747 sc-205747A | 10 g 25 g | $69.00 $110.00 | 4 | |
Antithyroid drug that may indirectly reduce THRβ1 activity by decreasing thyroid hormone synthesis. | ||||||
6-Propyl-2-thiouracil | 51-52-5 | sc-214383 sc-214383A sc-214383B sc-214383C | 10 g 25 g 100 g 1 kg | $36.00 $55.00 $220.00 $1958.00 | ||
Inhibits thyroid hormone synthesis, thereby indirectly reducing the activation of THRβ1. | ||||||
Amiodarone | 1951-25-3 | sc-480089 | 5 g | $312.00 | ||
Antiarrhythmic drug that can block thyroid hormone action and interfere with THRβ1 function due to its structural similarity to T4. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $62.00 $260.00 | 21 | |
Antifungal agent that can inhibit steroidogenesis, indirectly affecting thyroid hormone levels and THRβ1 activity. | ||||||
Lead(II) Acetate | 301-04-2 | sc-507473 | 5 g | $83.00 | ||
Lead(II) acetate can bind to the sulfhydryl groups of cysteine residues in proteins. If such a residue is critical in the ligand-binding domain or DNA-binding domain of c-Erb A β1, this interaction could inhibit the receptor′s function by preventing ligand binding or DNA interaction. | ||||||
Cadmium chloride, anhydrous | 10108-64-2 | sc-252533 sc-252533A sc-252533B | 10 g 50 g 500 g | $55.00 $179.00 $345.00 | 1 | |
Cadmium can displace metal ions that are cofactors in various enzymes and proteins, potentially changing the conformation of c-Erb A β1. This alteration can inhibit the receptor′s ability to bind to its ligand or to DNA, thus inhibiting its function. | ||||||
Rutaecarpine | 84-26-4 | sc-205846 sc-205846A | 10 mg 25 mg | $123.00 $359.00 | 1 | |
Alkaloid that has been shown to interfere with THRβ1 activity, possibly by affecting its expression or function. | ||||||
Proadifen hydrochloride | 62-68-0 | sc-200492 sc-200492A | 250 mg 1 g | $144.00 $421.00 | 1 | |
SKF-525A is a non-selective inhibitor of cytochrome P450 enzymes. By inhibiting these enzymes, it can reduce the synthesis of thyroid hormones, the natural ligands of c-Erb A β1, therefore indirectly inhibiting the receptor′s activation. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $76.00 $82.00 $367.00 | 36 | |
Synthetic glucocorticoid that may downregulate THRβ1 expression and reduce its transcriptional activity. | ||||||