c-Erb-A α-2 Activators
c-Erb-A α-2 Activators are a collection of chemical compounds that influence the functional activity of c-Erb-A α-2, a nuclear receptor that modulates the transcription of genes in response to thyroid hormones. Triiodothyronine (T3) is the endogenous ligand for c-Erb-A α-2, binding directly to the receptor and inducing transcriptional changes in responsive genes, representing the most direct form of activation. Other compounds, such as Tetraiodothyroacetic acid (tetrac) and thyroid hormone analogues like GC-1 (Sobetirome) and DITPA, also interact with c-Erb-A α-2, albeit with varying degrees of specificity and potency. These analogues maintain the key characteristic of promoting gene expression through the thyroid hormone response elements. Additionally, compounds like Tetrabromobisphenol A (TBBPA) and Resveratrol affect c-Erb-A α-2 activity, albeit through more indirect interactions with the receptor or its signaling pathways.
Moreover, some activators function through the formation of receptor heterodimers, as is the case with Bexarotene, an RXR agonist that indirectly promotes c-Erb-A α-2 activity by facilitating the formation of RXR/TR heterodimers essential for receptor-mediatedtranscription. Compounds like KB-141, CO23, and TRIAC, despite varying affinities and effects, all contribute to the modulation of thyroid hormone signaling, potentially impacting c-Erb-A α-2 functional activity. While compounds such as Selumetinib and AG 1478 do not directly target thyroid hormone receptors, they influence the broader signaling landscape in which c-Erb-A α-2 operates. By inhibiting MEK or EGFR tyrosine kinase activity respectively, these compounds may shift the signaling equilibrium in a way that indirectly enhances c-Erb-A α-2 signaling, leading to increased transcription of target genes. This diverse set of activators illustrates the multiple layers of regulation and the complexity of pathways that converge on the modulation of c-Erb-A α-2 activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
L-3,3′,5-Triiodothyronine, free acid | 6893-02-3 | sc-204035 sc-204035A sc-204035B | 10 mg 100 mg 250 mg | $40.00 $75.00 $150.00 | ||
Triiodothyronine or T3 is the active thyroid hormone that directly binds to c-Erb-A α-2, leading to the activation of its transcriptional activity. The binding of T3 to c-Erb-A α-2 results in conformational changes that allow the recruitment of coactivator proteins and the initiation of gene transcription. | ||||||
L-Thyroxine, free acid | 51-48-9 | sc-207813 sc-207813A | 100 mg 500 mg | $34.00 $73.00 | 2 | |
Thyroxine, also known as T4, is a prohormone that is converted to the active form T3 in target tissues. T4 can enhance the activity of c-Erb-A α-2 indirectly by being converted to T3, which then activates the receptor. | ||||||
9-cis-Retinoic acid | 5300-03-8 | sc-205589 sc-205589B sc-205589C sc-205589D sc-205589A | 1 mg 25 mg 250 mg 500 mg 5 mg | $70.00 $416.00 $3060.00 $5610.00 $145.00 | 10 | |
9-cis-Retinoic Acid is a retinoid that can bind to the retinoid X receptor (RXR), which heterodimerizes with the c-Erb-A α-2. This heterodimerization is essential for DNA binding and transcriptional regulation of thyroid hormone-responsive genes. | ||||||
Selumetinib | 606143-52-6 | sc-364613 sc-364613A sc-364613B sc-364613C sc-364613D | 5 mg 10 mg 100 mg 500 mg 1 g | $28.00 $80.00 $412.00 $1860.00 $2962.00 | 5 | |
Selumetinib is a MEK inhibitor that can indirectly enhance the activity of c-Erb-A α-2 by modulating downstream effects of the MAPK pathway, which can impact thyroid hormone signaling and c-Erb-A α-2-mediated transcription. | ||||||
Sodium Butyrate | 156-54-7 | sc-202341 sc-202341B sc-202341A sc-202341C | 250 mg 5 g 25 g 500 g | $30.00 $46.00 $82.00 $218.00 | 19 | |
Sodium Butyrate is a histone deacetylase inhibitor that can increase the acetylation of histones, leading to a more open chromatin structure. This can enhance c-Erb-A α-2's access to DNA and its transcriptional activity. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin activates adenylate cyclase, increasing cAMP levels and activating PKA. Activated PKA can phosphorylate proteins that interact with c-Erb-A α-2, potentially enhancing its transcriptional activity. | ||||||
Dibutyryl-cAMP | 16980-89-5 | sc-201567 sc-201567A sc-201567B sc-201567C | 20 mg 100 mg 500 mg 10 g | $45.00 $130.00 $480.00 $4450.00 | 74 | |
Dibutyryl cAMP is a cAMP analog that can permeate cell membranes and activate PKA. This activation can lead to enhanced c-Erb-A α-2 activity by promoting coactivator recruitment or modifying its phosphorylation state. | ||||||
Bexarotene | 153559-49-0 | sc-217753 sc-217753A | 10 mg 100 mg | $54.00 $245.00 | 6 | |
Bexarotene is a retinoid X receptor (RXR) agonist that can form heterodimers with c-Erb-A α-2. Activation of RXR by bexarotene can enhance the transcriptional activity of c-Erb-A α-2. | ||||||
Rosiglitazone | 122320-73-4 | sc-202795 sc-202795A sc-202795C sc-202795D sc-202795B | 25 mg 100 mg 500 mg 1 g 5 g | $118.00 $320.00 $622.00 $928.00 $1234.00 | 38 | |
Rosiglitazone is a PPARγ agonist that can heterodimerize with RXR, similar to c-Erb-A α-2. While not a direct activator, rosiglitazone may influence the transcriptional regulatory functions of c-Erb-A α-2 indirectly through its action on PPARγ. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium Chloride can inhibit glycogen synthase kinase-3 (GSK-3). Inhibition of GSK-3 may affect signaling pathways that interact with thyroid hormone signaling, potentially enhancing c-Erb-A α-2 activity. | ||||||