rxrβ

LG-100064 is an agonist of retinoid-X-receptor (RXR)(EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ)

AGN194204 (IRX4204) is inactive against RAR and is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 has anti-inflammatory and antic

RXR agonist 1 (Compound 33) is a highly selective RXR agonist, exhibiting EC50 values of 9 nM, 18 nM, and 11 nM for RXRα, RXRβ, and RXRγ, respectively. It demonstrates strong affinity for RXR with a Kd of 0.03 μM.

RXR agonist 3 (Compound 35) is a potent partial agonist of RXR, showing EC50 values of 3 nM for RXRα, 3 nM for RXRβ, and 8 nM for RXRγ. It is applicable in research related to Alzheimer's disease, multiple sclerosis, and lymphoma.

RXR agonist 2 (Compound 22) is a highly selective agonist of the retinoid X receptor (RXR) with an EC50 of 0.039 μM. It shows potential for use in research on metabolic syndrome and Alzheimer's disease.

RXR antagonist 6 (Compound 34) is a selective partial antagonist of the retinoid X receptor (RXR). It exhibits no agonistic activity on human RXRα/β/γ subtypes, but it effectively inhibits receptor activation induced by full RXR agonists such as Bezafibrate, with an IC50 value of 2.7 μM. Additionally, RXR antagonist 6 can enhance PMA-induced differentiation of THP-1 cells and is applicable in research related to cancer, metabolic disorders, and neurological diseases, including lymphoma.

Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR, with Ks values of 0.6 and 1.1 µM, respectively. It disrupts the stability of Nurr1 homodimers selectively while stabilizing Nurr1:RXR heterodimers, specifically activating the heterodimer response element DR5. In neuronal cells, Nurr1/RXR dual agonist 1 enhances the expression of neuroprotective Nurr1 target genes without inducing genes associated with off-target effects. This compound is applicable in studies related to neurodegenerative diseases.

RXR antagonist 1 is a Retinoid X Receptor (RXR) modulator that exhibits high RXR antagonism (pA2: 8.06). RXR antagonist 1 can be used to study type 2 diabetes.

RXR antagonist 2 is a potent antagonist of RXR (Ki: 0.391 μM, Kd: 0.281 μM). RXR antagonist 2 has shown research potential for RXR-related diseases.

(RXR)4XB is a cell-penetrating peptide that binds to phosphorodiamidate morpholino oligomer (PMO), resulting in a peptide-conjugated PMO (PPMO) and enhancing the delivery of PMO into bacterial cells. The (RXR)4XB-PMO conjugate prevents biofilm formation, inhibits Pseudomonas aeruginosa (with an MIC50 of 0.5-16 μM), and reduces bacterial load in a mouse acute pneumonia model.

(RXR)4XB TFA is a cell-penetrating peptide that binds phosphorodiamidate morpholino oligomer (PMO) to create a peptide-conjugated PMO (PPMO) for enhanced delivery into bacterial cells. The (RXR)4XB TFA-PMO complex inhibits biofilm formation, suppresses Pseudomonas aeruginosa with a MIC50 of 0.5-16 μM, and reduces bacterial load in a mouse acute pneumonia model.

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

K-8012 is a modulator of the N-terminally truncated RXRα and improves anticancer activities in an RXRα-dependent manner.

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

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

Acitretin (Ro 10-1670) is a second-generation systemic retinoid used in the treatment of psoriasis.

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

CD3254 is a selective and potent retinoid X receptor-like (RXR) agonist that inhibits neuronal cell death with OGD/reoxygenation.

PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1/Th2 development.

HX 531 is a RXR antagonist (IC50 of 18 nM). HX 531 prevents HF diet-induced obesity, insulin resistance, and diabetes by reducing tissue TG content in white adipose tissue (WAT), skeletal muscle, and liver in mice.

SR11237 is a Pan retinoid X receptor (RXR) agonist. SR11237 causes RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

Bigelovin is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.

Peretinoin (NIK333) is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as RXR and RAR.