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 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.

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.

TrxR-IN-8 (Compound 6f) is a selective inhibitor of TrxR with an IC50 of 10.2 μM. It induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species, reducing intracellular thiols, and lowering the glutathione/glutathione disulfide ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells.

TrxR-IN-6 (compound 1d) is an inhibitor of TrxR that can induce the accumulation of reactive oxygen species (ROS) and possesses anticancer properties. This compound can further lead to the collapse of the redox system, inducing mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and DNA damage. Ultimately, it triggers oxidative stress and induces apoptosis.