Molecular Formula | C28H36O4 |
Molar Mass | 436.58 |
Solubility | Soluble in DMSO |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
Use | UVI3003 is a RXR antagonist. It displays high RXR binding affinity. UVI3003 does not affect the corepressor interaction capacity of the RARα subunit within the context of the RAR-RXR heterodimer. |
Target | Xenopus RXRα, in Cos7 cells Human RXRα, in Cos7 cells |
In vitro study | UVI3003 inhibits the activity of xenopus and human RXRα, with IC 50 s of 0.22 and 0.24 μM, respectively. UVI3003 fully activates xPPARγ with an EC 50 of 12.6 μM, and is almost completely inactive on hPPARγ and mPPARγ. UVI 3003 (10 μM) does not change the proliferation rate of extraocular muscles (EOM)-derived or LEG-derived EECD34 cells. UVI 3003 causes a 65.4% difference in EECD34 cell fusion and desmin expression. |
Reference Show more | 1: Zhu J, Janesick A, Wu L, Hu L, Tang W, Blumberg B, Shi H. The unexpected teratogenicity of RXR antagonist UVI3003 via activation of PPARγ in Xenopus tropicalis. Toxicol Appl Pharmacol. 2017 Jan 1;314:91-97. doi: 10.1016/j.taap.2016.11.014. Epub 2016 Nov 25. PubMed PMID: 27894914; PubMed Central PMCID: PMC5183475. 2: Mihály J, Gericke J, Lucas R, de Lera AR, Alvarez S, Törőcsik D, Rühl R. TSLP expression in the skin is mediated via RARγ-RXR pathways. Immunobiology. 2016 Feb;221(2):161-5. doi: 10.1016/j.imbio.2015.09.013. Epub 2015 Sep 10. PubMed PMID: 26531761. 3: Zheng L, Yu J, Shi H, Xia L, Xin Q, Zhang Q, Zhao H, Luo J, Jin W, Li D, Zhou J. Quantitative toxicoproteomic analysis of zebrafish embryos exposed to a retinoid X receptor antagonist UVI3003. J Appl Toxicol. 2015 Sep;35(9):1049-57. doi: 10.1002/jat.3099. Epub 2015 Jan 11. PubMed PMID: 25581642. 4: Sun J, Narayanasamy S, Curley RW Jr, Harrison EH. β-Apo-13-carotenone regulates retinoid X receptor transcriptional activity through tetramerization of the receptor. J Biol Chem. 2014 Nov 28;289(48):33118-24. doi: 10.1074/jbc.M114.610501. Epub 2014 Oct 16. PubMed PMID: 25324544; PubMed Central PMCID: PMC4246072. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.291 ml | 11.453 ml | 22.905 ml |
5 mM | 0.458 ml | 2.291 ml | 4.581 ml |
10 mM | 0.229 ml | 1.145 ml | 2.291 ml |
5 mM | 0.046 ml | 0.229 ml | 0.458 ml |
biological activity | UVI 3003 is a highly selective inhibitor of retinoid X receptor (RXR), inhibition of xenopus toad and human rxrα activity, IC50 values were 0.22 and 0.24 μm. |
Target | IC50: 0.22 μm (Xenopus rxrα, in Cos7 cells), 0.24 μm (Human rxrα, in Cos7 cells) |
in vitro study | UVI3003 inhibitors the activity of xenopus and human rxrα, with IC 50 s of 0.22 and 0.24 μm. UVI3003 fully activated xPPAR gamma with an EC 50 of 12.6 μm, and is almost complete inactive on hPPARγ and mPPARγ. UVI 3003 (10 μM) does not change the proliferation rate of extraocular muscles (EOM)-derived or LEG-derived EECD34 cells. UVI 3003 causes a 65.4% difference in EECD34 cell fusion and desmin expression. |