retinoic

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.

9-cis-Retinoic Acid (Alitretinoin) is a derivative of vitamin A. It is a RAR/RXR agonist with anticancer, antitumor, anti-inflammatory, and neuroprotective activities, induces apoptosis, regulates the cell cycle, and can be used to study advanced tumors.

Retinoic acid-d5 (Vitamin A acid-d5) is the deuterium-labeled form of Retinoic acid. Retinoic acid is a natural RAR receptor agonist with an IC50 of 14 nM for RARα/β/γ and a Kd of 17 nM for PPARβ/δ. Retinoic acid, a metabolite of vitamin A, plays an important role in cell growth, differentiation and organ development. Retinoic acid acts by activating retinoic acid receptor alpha as an inhibitor of the transcription factor Nrf2.

all-trans-4-Oxoretinoic acid (all-trans 4-Keto Retinoic Acid) is an active metabolite of vitamin A.

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

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

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.

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.

LG-100064 is an agonist of retinoid-X-receptor (RXR)(EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ)

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

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.

(-)-Talarozole [formerly R115866] is a highly effective inhibitor of retinoic acid metabolism.

LY2955303 is an effective and selective antagonist of retinoic acid receptor gamma (RARγ, Ki = 1.09 nM).

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

Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression.

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.

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.

SR11237 is a Pan retinoid X receptor (RXR) agonist. SR11237 causes RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.

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.

CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.