Retinoid Receptor

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  1. Acitretin is a second generation retinoid and is typically used for psoriasis.
  2. Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions.
  3. Tazarotene is a prodrug and a member of the acetylenic class of retinoids.
  4. RAR agonist

    Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).
  5. Retinoid X Receptor Ligand

    Bexarotene is a highly selective retinoid X receptor (RXR) agonist.
  6. Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
  7. RARα agonist

    Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.
  8. RARα agonist

    AM 580 is an analog of retinoic acid that acts as a selective RARα agonist.
  9. RARγ-selective agonist

    CD 437 is a synthetic retinoid that is an RARγ-selective agonist.
  10. RAR agonist

    Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.
  11. Palovarotene is a novel retinoic acid receptor gamma agonist for the treatment of emphysema
  12. AR7

    RARα antagonist.

    AR7 was developed as a highly potent and selective enhancer of the chaperone-mediated autophagy (CMA) through antagonizing RARα.
  13. RAR agonist

    TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).
  14. RXR agonist

    LG 100268 is a potent RXR agonist for evaluation in the treatment of non-insulin-dependent (type II) diabetes mellitus (NIDDM).
  15. pan-RARs agonist

    AGN 194310 is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.
  16. RARα agonist

    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.
  17. RARα antagonist

    AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
  18. RAR agonist

    AGN 205327 is a potent synthetic RARs agonist with EC50 of 3766/734/32 nM for RARα/β/γ respectively; no inhibition on RXR.
  19. RARγ antagonist

    AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.
  20. Etretinate is a second-generation retinoid to treat severe psoriasis; has been replaced by acitretin, a safer metabolite of etretinate.
  21. RAR agonist

    WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist.
  22. antagonist of RXRα

    β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  23. RXR 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.
  24. RAR degrader

    PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
  25. RARγ antagonist

    LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.
  26. RXR antagonist

    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  27. Human RARβ2 receptor agonist

    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
  28. RARα agonist

    AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
  29. RAR agonist

    Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
  30. CYP26 inhibitor/RAMBA

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  31. retinoic acid metabolism inhibitor

    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  32. retinoic acid metabolism inhibitor

    (-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  33. RXRα antagonist

    β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
  34. RARβ agonist

    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist.
  35. RARγ-TNFAIP3 Activator

    ZSH-2208 is a retinoic acid A analog that exhibits potent antitumor activity against tumor regenerative stem cells (TRCs) in esophageal squamous cell carcinoma (ESCC). Its mechanism of action involves the RARγ–TNFAIP3 signaling pathway.
  36. RAR Agonist

    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.
  37. RXRa Antagonist

    K-8012 is a potent RXRa antagonist, with an IC50 of approximately 9.2 μM for inhibiting 9-cis-retinoic acid-induced Gal4-RXRa-LBD trans-activation. This compound demonstrates enhanced anticancer activity compared to sulindac in an RXRa-dependent manner. K-8012 effectively inhibits the tRXRa-mediated PI3K/AKT signaling pathway, promoting apoptosis and suppressing AKT activation by disrupting the interaction between tRXRa and p85α. These properties make K-8012 valuable for research in cancer biology and signaling pathways.
  38. Selective RXR Agonist

    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.
  39. RAR Agonist

    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.
  40. Rare Aldopentose

    D-Arabinopyranose is a rare aldo-pentose that serves as a precursor to D-arabinose in its open-chain form. This compound exhibits significant biological activity, including antidepressant effects and growth inhibition in Caenorhabditis elegans with an IC50 of 7.5 mM. D-Arabinose penetrates the blood-brain barrier, specifically modulating the metabolism of D-ribose and D-fructose, while also demonstrating antibacterial properties by inhibiting biofilm synthesis. Additionally, it activates the ACSS2-PPARγ/TFEB-CRTC1 axis via the lysosomal AXIN-LKB1-AMPK pathway, leading to antidepressant-like outcomes.
  41. RAR/RXR Agonist

    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.
  42. RXR Antagonist

    HX531 is an orally active antagonist of the retinoid X receptor (RXR), demonstrating an IC50 of 18 nM. This compound effectively upregulates the p53-p21Cip1 pathway while counteracting the anti-apoptotic effects of trans-retinoic acid (t-RA). HX531 is characterized by its potential applications in anti-obesity, anti-diabetic, and anti-melanoma research, making it a valuable tool for investigating metabolic and cancer-related pathways.
  43. RARα Antagonist

    Ro 41-5253 is a selective antagonist of the retinoic acid receptor alpha (RARα). It effectively binds to RARα without promoting transcriptional activity or influencing RAR/RXR heterodimerization and DNA binding. This compound demonstrates significant inhibition of cancer cell proliferation and can induce apoptosis, highlighting its potential as an antitumor agent in cancer research applications.
  44. RXR Agonist

    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.
  45. RARγ Inhibitor

    ZSH-512 is a potent inhibitor of retinoic acid receptor gamma (RARγ). It demonstrates significant antiproliferative effects by inducing apoptosis in cancer cells, while concurrently downregulating key stemness markers such as CD133, NANOG, SOX2, and EPCAM. With its strong anticancer activity, ZSH-512 is a valuable tool for investigating therapeutic strategies in colorectal cancer research.
  46. RARγ Agonist

    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.
  47. RXR Agonist

    Bexarotene-d4 is a deuterium-labeled analog of Bexarotene, functioning as a selective retinoid X receptor (RXR) agonist. This compound is primarily utilized in the treatment of cutaneous T-cell lymphoma, demonstrating significant biological activity in modulating RXR signaling pathways. Its isotopic labeling facilitates research applications in pharmacokinetics and metabolism studies of RXR-targeted therapies.
  48. RAR/RXR

    Ch55-O-C3-NH2 is a selective ligand for retinoic acid receptors (RAR) and retinoid X receptors (RXR). This compound demonstrates the ability to effectively modulate RAR signaling pathways, facilitating research into their role in gene expression and developmental processes. Ch55-O-C3-NH2 can also be utilized in the synthesis of SNIPERs by binding to cIAP1 ligand Bestatin through a linker, supporting studies in targeted protein degradation and therapeutic applications.
  49. RAR/RXR Agonist

    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.
  50. RAR Agonist

    Retinoic acid-d5 is a deuterium-labeled derivative of retinoic acid, functioning as a selective retinoic acid receptor (RAR) agonist. It is crucial for cellular processes such as growth, differentiation, and organogenesis, demonstrating IC50 values of 14 nM for RARα, β, and γ subtypes. Additionally, retinoic acid-d5 interacts with the peroxisome proliferator-activated receptor β/δ (PPARβ/δ) with a Kd of 17 nM and inhibits the transcription factor Nrf2 through RARα activation. This compound is essential for studies involving retinoid signaling and cell differentiation.

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