nuclear receptor

SR-29065 is a selective REV-ERBα agonist that inhibits BMAL1 transcription within the circadian transcription–translation feedback loop, and it has been applied to evaluate whether targeting both negative regulatory limbs of circadian control yields synergistic anti-tumor effects in glioblastoma models, supporting its broader use in autoimmune disorder and circadian rhythm research.

7α-(Thiomethyl)spironolactone is a nuclear steroid receptor antagonist and a major metabolite of the synthetic steroid spironolactone. 7α-(Thiomethyl)spironolactone is used in pharmacological studies, including research on steroid metabolism, nuclear receptor signaling, and coronavirus-related investigations.

SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor with a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, without affecting the nuclear translocation of p65 mediated by the TNF-α receptor. It inhibits p52 nuclear translocation stimulated by TWEAK or Anti-LTβR with an IC50 of 10 μM and regulates the NF-kB signaling pathway in a ligand-independent manner.

Dicirenone (SC26304) inhibits the Mineralocorticoid receptor (MR), aldosterone regulation of the urinary K+:Na+ ratio, and aldosterone binding to renal cytoplasmic and nuclear receptors.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.

PF-02413873 is a competitive antagonist of nonsteroidal progesterone receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.

KRM-III is an orally active T cell antigen receptor (TCR) inhibitor with anti-inflammatory activity that potently inhibits TCR and myristate acetate/fosfomycin/ionomycin-induced NFAT nuclear factor activation and T cell proliferation, with an IC50 of approximately 5 μM.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1/2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

Lem-14-1189, a LEM-14 derivative, is a potent NSD inhibitor of the nuclear receptor binding SET domain, and has inhibitory effects on NSD1, NSD2, and NSD3, with IC50 of 418 μM, 111 μM, and 60 μM, respectively. LEM-14-1189 has potential anticancer activity and can be used to study multiple myeloma (MM) and diseases of the blood system.

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.

Beclometasone dipropionate (Vancenase) is the dipropionate ester of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production.

Articaine hydrochloride (Hoe-045), a thiophene-containing local anesthetic, is pharmacologically similar to mepivacaine.

AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].

Sinomenine (Kukoline) is a pure alkaloid isolated from the Sinomenium acutum, is utilized in the treatment of rheumatism and arthritis.

Baicalin (Baicalein 7-O-β-D-glucuronide) is a prolyl endopeptidase inhibitor isolated from scutellaria baicalensis, with antioxidant, anti-tumor, anti-HIV properties.

Ginsenoside Rb1 (Gypenoside Ⅲ) is part of a class of steroid glycosides; may have properties that inhibit or prevent the growth of tumors.