retinoid receptor

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.

K-8012 is a modulator of the N-terminally truncated RXRα and improves anticancer activities in an RXRα-dependent manner.

Oxybenzone is a UV filter commonly used in tanning and skin protection agents. It is a derivative of benzophenone and is used as an endocrine disrupting chemical that penetrates the placental and blood-brain barriers. It impairs autophagy, alters epigenetic status and disrupts vitamin X-like receptor signaling in apoptotic neuronal cells.

Etodolac (AY-24236) inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα/β/γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

Acitretin (Ro 10-1670) is a second-generation systemic retinoid used in the treatment of psoriasis.

Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs), which act as transcription factors that promote cell differentiation and apoptosis. This naturally occurring retinoic acid has potential antineoplastic activity, exhibits immunomodulatory and anti-inflammatory responses, and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Tamibarotene (Amnolake) is an orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity.

Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.

AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.

TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.

AC-55649 is a potent and highly isoform-selective agonist of the human RARβ2 receptor, characterized by a pEC50 of 6.9.

CD2665 is an orally active antagonist of retinoic acid receptor (RAR). For RARγ and RARβ, the Kis are 110 nM and 306 nM.

CD3254 is a selective and potent retinoid X receptor-like (RXR) agonist that inhibits neuronal cell death with OGD/reoxygenation.

PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1/Th2 development.

Fenretinide (4-HPR) is an orally-active synthetic retinoid derivative with potential antineoplastic and chemopreventive activities.

BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.

Luffariellolide is a terpene compound obtained from the marine sponge Hyrtios communis. It is an inhibitor of human synoviocyte protein phospholipase A2 (HSF-PLA2) and a retinoic acid receptor (RAR) agonist. Luffariellolide inhibits hypoxia (1% O2)-induced HIF-1 activation and inhibits cell growth.

BMS 753 is an agonist of isotype-selective retinoic acid receptor α (RARα, Ki= 2 nM).

BMS 195614 (BMS614) is a selective RARα antagonist. BMS 195614 can bind to the RARα subunit.

HX 531 is a RXR antagonist (IC50 of 18 nM). HX 531 prevents HF diet-induced obesity, insulin resistance, and diabetes by reducing tissue TG content in white adipose tissue (WAT), skeletal muscle, and liver in mice.

BMS270394 is a RARγ agonist used in the study of breast cancer and dermatologic diseases.

Ro 41-5253 is an orally active RARα antagonist, ligand, and partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. It exhibits antitumor activity, inhibits proliferation, and induces apoptosis in MCF-7 and ZR-75.1 estrogen receptor-positive breast cancer cells.