rar/rxr

Compound 7, also known as RAR RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2 M arrest and apoptosis in cancer cells.

BMS-185354 is a selective RARγ activator with an EC50 value of 28 nM, offering potential for cancer research.

ZSH-2208, an analogue of retinoic acid A, exerts strong anti-tumor effects on regenerative stem cells (TRCs) in esophageal squamous cell carcinoma (ESCC) via the RARγ-TNFAIP3 pathway.

DC360 is a synthetic analog of all-trans retinoic acid (ATRA) that can induce the expression of RARβ. It is useful for studies characterizing the retinoic acid signaling pathway.

IRX5010 (IRX4647F), an analogue of IRX4647, serves as a highly selective RARγ nuclear receptor agonist. It effectively inhibits the growth of EMT-6 triple-negative breast cancer.

ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

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.

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

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

K-80003(TX-803) is a potent retinol-like X-receptor-alpha regulator that inhibits TRxrα-dependent Akt activation and tumor cell growth.

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.

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

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.

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.

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.

LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist that agonizes RXR-α, RXR-β, and RXR-γ at the nanomolar level, selectively exceeding the RAR by three orders of magnitude.LG100268 is capable of inducing transcriptional activation in adipocytes; affecting the RXRs and their chaperone receptor, Foxl2 Dmrt1, to induce flounder masculinization in juvenile flounder; inhibits keratin 17 expression in nigrostriatal epithelial cells; and increases PD-L1 expression in HER2 or triple-negative breast cancer.

UVI 3003 is a highly selective antagonist of the retinoid X receptor, inhibiting Xenopus and human RXRα in Cos7 cells with IC50 values of 0.22 μM and 0.24 μM, respectively.

AM580 (CD336) is a retinoic acid receptor agonist that is selective for RARα( IC50 : 8 nM )