ERRα

ERRα is an orphan nuclear receptor first identified by homology to steroid hormone receptors, and it functions as a transcriptional regulator rather than an estrogen receptor^[1]. Mechanistically, ERRα works with PGC-1α to activate mitochondrial genes, oxidative phosphorylation, and mitochondrial biogenesis^[2]^[3]. In cardiac and skeletal muscle, ERRα directs PPARα-linked transcriptional control of fatty-acid transport and cellular energy metabolism^[4]. In brown adipose tissue models, loss of ERRα impairs mitochondrial oxidative metabolism and adaptive thermogenesis, supporting its use in metabolic research models^[5]. Disease-focused studies connect ERRα activity with breast cancer heterogeneity and negative prognosis, while metabolic studies position ERRα as a regulator of high-energy cellular states^[6]. Compared with related isoforms, ERRα and ERRγ mainly regulate metabolic genes, whereas ERRβ is more closely linked to embryonic stem-cell pluripotency^[7]. For experimental applications, the inverse agonist XCT790 disrupts PGC-1α/ERRα signaling, and the synthetic pan-ERR agonist SLU-PP-332 activates an ERRα-dependent aerobic exercise program in skeletal muscle^[8]^[9].

References:

[1]. Giguère V, et al. Identification of a new class of steroid hormone receptors. Nature. 1988 Jan 7;331(6151):91-4. [Content Brief]

[2]. Schreiber SN, et al. The estrogen-related receptor alpha (ERRalpha) functions in PPARgamma coactivator 1alpha (PGC-1alpha)-induced mitochondrial biogenesis. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6472-7. [Content Brief]

[3]. Mootha VK, et al. Erralpha and Gabpa/b specify PGC-1alpha-dependent oxidative phosphorylation gene expression that is altered in diabetic muscle. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6570-5. [Content Brief]

[4]. Huss JM, et al. Estrogen-related receptor alpha directs peroxisome proliferator-activated receptor alpha signaling in the transcriptional control of energy metabolism in cardiac and skeletal muscle. Mol Cell Biol. 2004 Oct;24(20):9079-91. [Content Brief]

[5]. Villena JA, et al. Orphan nuclear receptor estrogen-related receptor alpha is essential for adaptive thermogenesis. Proc Natl Acad Sci U S A. 2007 Jan 23;104(4):1418-23. [Content Brief]

[6]. Deblois G, et al. Genome-wide identification of direct target genes implicates estrogen-related receptor alpha as a determinant of breast cancer heterogeneity. Cancer Res. 2009 Aug 1;69(15):6149-57. [Content Brief]

[7]. Huss JM, et al. Constitutive activities of estrogen-related receptors: Transcriptional regulation of metabolism by the ERR pathways in health and disease. Biochim Biophys Acta. 2015 Sep;1852(9):1912-27. [Content Brief]

[8]. Willy PJ, et al. Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand. Proc Natl Acad Sci U S A. 2004 Jun 15;101(24):8912-7. [Content Brief]

[9]. Billon C, et al. Synthetic ERRα/β/γ Agonist Induces an ERRα-Dependent Acute Aerobic Exercise Response and Enhances Exercise Capacity. ACS Chem Biol. 2023 Apr 21;18(4):756-771. [Content Brief]

ERRα Related Products (11)
Antibodies (2)

ERRα Related Products (11):

By Type:	Pan (2) Selective (5)
By Effects:	Inhibitors (2) Agonists (3) Antagonists (4) Activator (1) Degrader (1)

Cat. No.	Product Name	Effect	Purity

HY-10426

XCT790	Antagonist	99.67%
XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

HY-155673

SLU-PP-332	Agonist	98.98%
SLU-PP-332 is a pan-Estrogen Receptor/ERR agonist with EC₅₀ values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function.

HY-113960

ERRα antagonist-1	Antagonist	99.71%
ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC₅₀ values are 170 nM and 180 nM, respectively.

HY-132205

DS45500853	Agonist	99.18%
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC₅₀ value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

HY-139185

PROTAC ERRα Degrader-3	Inhibitor	98.82%
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.

HY-180961

His-TERRα	Degrader
His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer.

HY-143201

DS20362725	Agonist	99.34%
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC₅₀ value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

HY-U00425

PROTAC ERRα ligand 1	Antagonist	98.61%
PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC₅₀ values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα^c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity.

HY-128838

PROTAC ERRα Degrader-1	Inhibitor	98.22%
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.

HY-144699

ERRα antagonist-2	Antagonist	99.07%
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC₅₀ of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.

HY-W020788

Benoxacor	Activator	99.39%
Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.

Name
Email *

	Sorry, but the email address you supplied was invalid.

ERRα

ERRα Related Products (11)

Antibodies (2)

ERRα Related Products (11):