rarα

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

AGN 194078 is a selective RARα agonist with a dissociation constant (Kd) of 3 nM and an effective concentration (EC50) of 112 nM.

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.

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

AGN 196996 is a potent and selective inhibitor of RARα (Ki: 2 nM), exhibiting very low affinity for RARβ (Ki: 1087 nM) and RARγ (Ki: 8523 nM).

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.

AGN 194310 (VTP-194310) is a pan-antagonist for retinoic acid receptors (RARs), with Kd values of 3 nM, 2 nM, and 5 nM for RARα, RARβ, and RARγ, respectively[1][2].

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.

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].

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).

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

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.