rxr

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

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.

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

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 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.

TrxR-IN-3 (Compound 2c) is an effective TrxR inhibitor that exhibits strong antiproliferative activities against five human cancer cell lines, particularly breast tumor cells. It increases ROS levels, induces apoptosis by regulating apoptosis-related protein expression in breast cancer cells, and promotes autophagosome and autolysosome formation by enhancing LC3-II and Beclin-1 expression and reducing LC3-I and p62 protein expression [1].

TrxR-IN-2 is a potential thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 has research value in the chemotherapy of drug-resistant hepatocellular carcinoma.

TrxR-IN-D9 is a novel inhibitor of thioredoxin reductase (TrxR).

TrxR-IN-5 (compound 4f) is an efficacious inhibitor of TrxR (thioredoxin reductase) with an IC50 of 0.16 μM. By elevating the levels of reactive oxygen species (ROS), TrxR-IN-5 fosters robust antiproliferative impacts and demonstrates pronounced effects against cancer proliferation and metastasis [1].

Compound 1b (TrxR-IN-4) is a potent TrxR inhibitor that activates endoplasmic reticulum stress (ERS) to induce apoptosis in HepG2 cells and mitigates CCl4-induced liver damage in vivo through TrxR expression down-regulation and reduced inflammation [1].

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.

TrxR1-IN-B19 (TrxR1 IN B19), a TrxR1 inhibitor, selectively kills gastric cancer cells by a small molecule via targeting TrxR1 and ROS-mediated ER stress activation.

Compound 5j, also known as TrxR1-IN-1, is a TrxR1 inhibitor with an IC50 of 8.8 μM. It exhibits anticancer activity, demonstrating IC50 values of 1.5 μM in MCF-7, 1.7 μM in HeLa, 2.4 μM in BGC-823, 2.8 μM in SW-480, and 2.1 μM in A549 cells. Additionally, TrxR1-IN-1 possesses antioxidant activity, effectively scavenging the DPPH radical [1].

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.

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

Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene. Fluorobexarotene  is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

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

Etodolac (AY-24236) inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.

Tamibarotene (Amnolake) is an orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity.

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα β γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

Oxybenzone is a UV filter commonly used in tanning and skin protection agents. It is a derivative of benzophenone and is used as an endocrine disrupting chemical that penetrates the placental and blood-brain barriers. It impairs autophagy, alters epigenetic status and disrupts vitamin X-like receptor signaling in apoptotic neuronal cells.