1. Signaling Pathways
  2. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  3. RAR/RXR

RAR/RXR

Retinoic acid receptors; Retinoid X receptors

The nuclear retinoic acid receptors (RARs) are transcriptional transregulators, which control the expression of specific gene subsets subsequently to ligand binding and to strictly controlled phosphorylation processes. RARs consist of three subtypes, α (NR1B1), β (NR1B2) and γ (NR1B3), encoded by separate genes. RARs function as ligand-dependent transcriptional regulators, heterodimerized with retinoid X receptors (RXRs), which also consist of three types, α NR2B1, β (NR2B2) and γ (NR2B3). RARs play critical roles in a variety of biological processes, including development, reproduction, immunity, organogenesis and homeostasis, as assessed by vitamin A-deficiency (VAD), pharmacological and genetic studies conducted in the mouse.

Retinoid X receptor (RXR) belongs to a family of ligand-activated transcription factors that regulate many aspects of metazoan life. A class of nuclear receptors requires RXR as heterodimerization partner for their function.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-160212
    JP3000
    Agonist
    JP3000 is agonist of RXRA, RXRB, RXRG.
    JP3000
  • HY-118364
    AGN 190727
    AGN 190727 is a structural isomer of AGN 190121 and has no activating effect on RAR/RXR. AGN 190121 is a RAR-specific agonist that causes a dose-dependent increase in serum triglycerides, leading to hypertriglyceridemia.
    AGN 190727
  • HY-B0091A
    Adapalene sodium salt
    Agonist
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
    Adapalene sodium salt
  • HY-118420
    BMS-185411
    Antagonist
    BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM.
    BMS-185411
  • HY-B0107A
    Acitretin sodium
    Agonist
    Acitretin (Ro 10-1670) sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin sodium also can be used for the research of Alzheimer’s disease.
    Acitretin sodium
  • HY-16685
    AGN 205327
    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.
    AGN 205327
  • HY-14171R
    Bexarotene (Standard)
    Agonist
    Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
    Bexarotene (Standard)
  • HY-15127S
    Isotretinoin-d5
    Agonist
    Isotretinoin-d5 is the deuterium labeled Isotretinoin. Isotretinoin is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity[1][2][3].
    Isotretinoin-d<sub>5</sub>
  • HY-121435
    K-8012
    Antagonist
    K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a.
    K-8012
  • HY-107218
    11-Hydroxysugiol
    Modulator
    11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).
    11-Hydroxysugiol
Cat. No. Product Name / Synonyms Application Reactivity

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