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Submit ReviewPA 452 is an RXR antagonist (pA2 = 7.11). Triggers dissociation of RXR tetramers. Attenuates cell proliferation and induces apoptosis in MCF-7 breast cancer cells.
M. Wt | 439.59 |
Formula | C26H37N3O3 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 457657-34-0 |
PubChem ID | 9803242 |
InChI Key | JJUUTJCZMGZJDZ-UHFFFAOYSA-N |
Smiles | CC1(C)C2=C(C=C(N(C3=NC=C(C(O)=O)C=N3)C)C(OCCCCCC)=C2)C(C)(C)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 43.96 | 100 | |
ethanol | 4.4 | 10 |
The following data is based on the product molecular weight 439.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.27 mL | 11.37 mL | 22.75 mL |
5 mM | 0.45 mL | 2.27 mL | 4.55 mL |
10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
References are publications that support the biological activity of the product.
Yasmin et al (2010) Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's oligomeric switch. J.Mol.Biol. 397 1121 PMID: 20188110
Takahashi et al (2002) Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions. J.Med.Chem. 45 3327 PMID: 12139443
Nakayama et al (2011) Discovery of a potent retinoid X receptor antagonist structurally closely related to RXR agonist NEt-3IBIB. J.Med.Chem.Lett 2 896 PMID: 24900278
If you know of a relevant reference for PA 452, please let us know.
Keywords: PA 452, PA 452 supplier, PA452, RXR, tetramers, retinoid, X, receptors, antagonists, Retinoid, Receptor, 5086, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PA 452 include:
Yuan et al (2018) A Chimeric Humanized Mouse Model by Engrafting the Human Induced Pluripotent Stem Cell-Derived Hepatocyte-Like Cell for the Chronic Hepatitis B Virus Infection. Front Microbiol 9 908 PMID: 29867819
Wang et al (2017) Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation. J Mol Cell Biol 9 338 PMID: 28992291
Do you know of a great paper that uses PA 452 from Tocris? Please let us know.
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