10 products were found matching "Cay16020"!

PGF2alpha is a widely distributed prostaglandin occurring in many species. It causes contraction of vascular, bronchial, intestinal, and myometrial smooth muscle, and also exhibits potent luteolytic activity. PGF2alpha exhibits its receptor mediated physiological activity at 50-100 nM. Maximal ovine myometrial...

BMS 195614 is a neutral retinoic acid receptor (RAR) alpha-selective antagonist (Ki = 2.5 nM). It antagonizes agonist-induced coactivator recruitment and moderately decreases SMRT binding to RAR but does not significantly affect nuclear receptor corepressor binding.Formal Name:...

CITCO is an agonist of human CAR (EC50 = 49 nM). It induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes, including several cytochrome P450 isoforms. CITCO less potently activates human pregnane X receptor (EC50 = 3 µM) and has no detectable activity on...

PHTPP is a pyrazolo[1,5-alpha]pyrimidine-based ligand that acts as a full antagonist of estrogen ERbeta receptors with 36-fold selectivity over ERalpha. It exhibits no significant agonism on ERalpha or ERbeta. This compound has been used to selectively target ERbeta in the study of the opposing effects of hormone...

Prostaglandin F2alpha diethyl amide (PGF2alpha-NEt2) is an analog of PGF2alpha (Cay-16010) in which the C-1 carboxyl group has been modified to an N-diethyl amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative PG hypotensive prodrugs. Studies...

UVI3003 is a full antagonist of RXR that demonstrates potent, nanomolar binding affinity. At 1 µM, UVI3003 does not affect the corepressor interaction capacity of the RARalpha subunit in the RAR-RXR heterodimer configuration. This compound can be used to isolate the contribution of RXR to the function of RXR...

Tomatine is a steroidal saponin that has been found in S. lycopersicum and has diverse biological activities. It is active against a panel of 19 plant pathogenic fungi (EC50s = 13-912 µM) and inhibits the growth of L. amazonensis promastigotes (IC50 = 124 nM). Tomatine (0.75, 1, and 1.5 µM) inhibits autophagy and...

3,3',5-Triiodo-L-thyronine (T3) is a thyroid hormone. It is produced by 5'-monodeiodination of the prohormone thyroxine (T4) in various tissues, including liver and kidney. T3 is an agonist of thyroid hormone receptors TRalpha and TRbeta (Kis = 2.3 nM for both) that modulates diverse biological properties, including...

Aldehyde dehydrogenase (ALDH) is an enzyme that catalyzes the oxidation of various aldehydes to their corresponding carboxylic acid. There are 19 human ALDH isozymes, which have varying expression levels, subcellular localization, tissue distribution, cofactor preference, and substrate specificity. ALDH exists as a...

Ciclopirox is an iron chelator, antifungal, and anticancer agent. It inhibits the iron-dependent enzyme hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2, IC50 = 1.58 µM), an effect that is reduced in the presence of iron. It stabilizes hypoxia-inducible factor-alpha (HIF-1alpha) under normoxic conditions in...