retinoidreceptor

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.

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

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.

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

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

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

Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of tumors and respiratory diseases.Mofarotene is a retinoic acid analog that binds to and activates retinoic acid receptors (RARs), which alters the expression of certain genes, leading to reduced cell differentiation and cell proliferation in susceptible cells.

KCL-286 is an orally available and potent retinoic acid receptor beta agonist for the amelioration of spinal cord injury (SCI).

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

1,3,5-Triisopropylbenzene is a benzene ring derivative commonly used in fuels, lubricants, and micellar expanders, and can be used as a potential retinoid X nuclear receptor alpha (RXRα) agonist (Activity Value=15µM).

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

ER-50891 is a potent retinoic acid receptor alpha (RARα) antagonist. er-50891 reduces the inhibitory effect of allosteric retinoic acid and restores osteoblast differentiation induced by bone morphogenetic protein 2.

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.

Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene. Fluorobexarotene  is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

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.

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

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.

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

Ch55 (3,5-Di-tert-butylchalcone) is an effective inducer of the differentiation of HL60 cells (EC50 = 200 nM) and shows high affinity with RAR-α and RAR-β receptors. Ch55 can be used in studies about cancer.

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.

AR7 is a retinoic acid receptor α (RARα) antagonist.

Tazarotene (Zorac) is a synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.

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