rarα

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

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

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.

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.

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.

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.

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

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

Compound 21, an orally active and selective RARα antagonist, exhibits a potent inhibition of the retinoic acid receptor α with an IC50 of 4.6 nM [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.

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

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.

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.

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

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.

Trifarotene (CD5789) is a potent and selective RARγ agonist, exhibiting 65-fold and 16-fold selectivity for RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).

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

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.

Piclamilast (RP 73401) is a PDE4 inhibitor.

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

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.

Bigelovin is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.