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Retinoid receptor ligands act on retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Both are nuclear receptors with α, β and γ subtypes that bind DNA as RAR-RXR heterodimers and regulate gene transcription. A receptor for the morphogen retinoic acid was identified in 1987 as a member of the nuclear receptor family. In 1990 a second receptor responding to retinoic acid, later named RXRα, revealed a distinct retinoid pathway. Tretinoin, the all-trans form of retinoic acid, activates RARs, while tamibarotene and AM 580 favor RARα and CD 437 favors RARγ. Adapalene, tazarotene, acitretin and fenretinide are synthetic retinoids, whereas bexarotene is a ligand selective for RXRs.
Synonyms: Retinoic Acid; ATRA; Vitamin A Acid
Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).
Synonyms: LGD 1069; SR 11247; Ro 26-4455; Targretin; LG 100069
Bexarotene is a highly selective retinoid X receptor (RXR) agonist.
Synonyms: Am80
Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.
Synonyms: CD 336; NSC 608001; Ro 40-6055
AM 580 is an analog of retinoic acid that acts as a selective RARα agonist.
Synonyms: AHPN
CD 437 is a synthetic retinoid that is an RARγ-selective agonist.
Synonyms: 4-HPR; (4-Hydroxyphenyl)retinamide
Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.
Palovarotene is a novel retinoic acid receptor gamma agonist for the treatment of emphysema
Synonyms: Arotinoid acid; Ro 13-7410
TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).
Synonyms: IRX4204; NRX194204; VTP 194204
AGN194204 is a selective retinoid X receptor (RXR) agonist with high affinity, exhibiting Kd values of 0.4 nM, 3.6 nM, and 3.8 nM for RXRα, RXRβ, and RXRγ, respectively, and EC50 values of 0.2 nM, 0.8 nM, and 0.08 nM. This compound is devoid of activity against retinoic acid receptors (RAR). AGN194204 demonstrates significant anti-inflammatory and anticarcinogenic properties, making it a valuable tool for research in inflammation and cancer biology.
Synonyms: AGN 192620; ALRT 268,CD 3127; LG 268; LGD 100268; LGD 1268
LG 100268 is a potent RXR agonist for evaluation in the treatment of non-insulin-dependent (type II) diabetes mellitus (NIDDM).
Synonyms: VTP194310
AGN 194310 is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.
AGN 195183 is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.
AGN 205327 is a potent synthetic RARs agonist with EC50 of 3766/734/32 nM for RARα/β/γ respectively; no inhibition on RXR.
Synonyms: CD 271 sodium salt
Adapalene sodium salt is a potent retinoic acid receptor (RAR) agonist, demonstrating significant binding affinity with AC50 values of 2.3 nM for RARβ, 9.3 nM for RARγ, and 22 nM for RARα. This third-generation synthetic retinoid is primarily utilized in acne research but has also been identified to inhibit the enzymatic activity of glutamate oxaloacetate transaminase 1 (GOT1) in a non-competitive manner. Additionally, adapalene sodium salt exhibits anti-tumor activity, making it valuable for diverse biological studies.
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist.
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
Synonyms: CD5789
Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
Synonyms: BMS-189453
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist.
Synonyms: AGN 190205; BASF-46928
EC23 is a retinoid analogue that acts as a retinoic acid receptor (RAR) agonist. This compound prompts neuronal differentiation, making it a valuable tool for studying neurodevelopmental processes and related disorders. Its stability enhances its suitability for various biological assays and research applications in the field of neurobiology.
Synonyms: Alitretinoin
9-cis-Retinoic acid is a potent RAR/RXR agonist derived from vitamin A. It plays a critical role in inducing apoptosis and regulating the cell cycle, exhibiting significant anticancer, anti-inflammatory, and neuroprotective activities. This compound is valuable for research applications aimed at understanding retinoid signaling and its implications in various biological processes and diseases.
HX630 is a potent retinoic acid X receptor (RXR) agonist that effectively induces apoptosis and exhibits significant anti-tumor activity. It is particularly valuable in the study of Cushing's disease and related tumorigenic processes. Research applications include elucidating the mechanisms of RXR activation and its therapeutic potential in cancer treatments.
CD1530 is a selective agonist of retinoic acid receptor gamma (RARγ) with notable antibacterial properties. It effectively decreases the phosphorylation of Smad1/5/8 and overall Smad levels, leading to a reduction in β-catenin, MMP9 protein, and reactive oxygen species (ROS) levels. CD1530 is utilized in research focusing on orthopedic conditions, such as heterotopic ossification and Achilles tendon injuries, as well as muscle disorders related to fatty infiltration.
Synonyms: Ro 10-1670 sodium
Acitretin sodium functions as a retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. Primarily utilized in the treatment of psoriasis, this second-generation systemic retinoid also shows potential in the research of Alzheimer's disease. Its ability to modulate gene expression and influence cellular differentiation makes it a valuable tool for investigating retinoid signaling pathways in various biological contexts.
