RXRα Antagonist

ER 50891 is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis.

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC₅₀ value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC₅₀ of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma.

AGN 193109 sodium is the sodium salt form of AGN 193109 (HY-U00449). AGN 193109 sodium is the pan antagonist for retinoic acid receptor (RAR), with K_d of 2, 2 and 3 nM, for RARα, RARβ and RARγ, respectively. AGN 193109 sodium reverses TTNPB-induced morphology changes and all-trans retinoic acid (tRA)/9-cis RA/13-cis RA-induced proliferation suppression in ECE16-1 cell. AGN 193109 sodium is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

(E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer.