rxr

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.

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.

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

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.

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 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 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.

Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.

(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.

TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1, demonstrating significant antitumor activity in nude mice and NSCLC organoids.

TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).

TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.