rarβ

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.

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).

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

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).

BMS641 (BMS-209641) is a selective and potent RARβ agonist with high affinity for RARβ, which synergistically activates RARβ and RARgamma to induce cellular maturation into specialized neuronal subtypes.

AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.

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

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].

CD2665 is an orally active antagonist of retinoic acid receptor (RAR). For RARγ and RARβ, the Kis are 110 nM and 306 nM.

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.

LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor activator with EC50s of 2.5 μM and 20 μM, respectively.

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.

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.

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.

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.

Ch55-O-C3-NH2, also known as RAR ligand 1, is a ligand derived from the Ch55 compound that specifically targets RAR. Through a linker, Ch55-O-C3-NH2 interacts with cIAP1 ligand Bestatin to form SNIPER[1].