PA 452

RXR antagonist CAS# 457657-34-0

PA 452

Catalog No. BCC8005----Order now to get a substantial discount!

Product Name & Size Price Stock
PA 452: 5mg $138 In Stock
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Quality Control of PA 452

Number of papers citing our products

Chemical structure

PA 452

3D structure

Chemical Properties of PA 452

Cas No. 457657-34-0 SDF Download SDF
PubChem ID 9803242 Appearance Powder
Formula C26H37N3O3 M.Wt 439.59
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 40 mg/mL (90.99 mM; Need ultrasonic and warming)
Ethanol : 4.4 mg/mL (10.01 mM; Need ultrasonic and warming)
Chemical Name 2-[(3-hexoxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-methylamino]pyrimidine-5-carboxylic acid
SMILES CCCCCCOC1=C(C=C2C(=C1)C(CCC2(C)C)(C)C)N(C)C3=NC=C(C=N3)C(=O)O
Standard InChIKey JJUUTJCZMGZJDZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H37N3O3/c1-7-8-9-10-13-32-22-15-20-19(25(2,3)11-12-26(20,4)5)14-21(22)29(6)24-27-16-18(17-28-24)23(30)31/h14-17H,7-13H2,1-6H3,(H,30,31)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PA 452

DescriptionRXR antagonist (pA2 = 7.11). Triggers dissociation of RXR tetramers. Attenuates cell proliferation and induces apoptosis in MCF-7 breast cancer cells.

PA 452 Dilution Calculator

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PA 452 Molarity Calculator

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Preparing Stock Solutions of PA 452

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2748 mL 11.3742 mL 22.7485 mL 45.4969 mL 56.8712 mL
5 mM 0.455 mL 2.2748 mL 4.5497 mL 9.0994 mL 11.3742 mL
10 mM 0.2275 mL 1.1374 mL 2.2748 mL 4.5497 mL 5.6871 mL
50 mM 0.0455 mL 0.2275 mL 0.455 mL 0.9099 mL 1.1374 mL
100 mM 0.0227 mL 0.1137 mL 0.2275 mL 0.455 mL 0.5687 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PA 452

Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB.[Pubmed:24900278]

ACS Med Chem Lett. 2011 Sep 27;2(12):896-900.

We discovered a potent retinoid X receptor (RXR) antagonist, 6-[N-ethyl-N-(5-isobutoxy-4-isopropyl-2-(E)-styrylphenyl)amino]nicotinic acid (13e), that is structurally closely related to the RXR full agonist 6-[N-ethyl-N-(3-isobutoxy-4-isopropylphenyl)amino]nicotinic acid (NEt-3IB) (4). Compound 13e was synthesized via a simple route from 11, a methyl ester precursor of 4. Because 11 possesses high electrophilic reactivity because of the amino and alkoxy groups, it was readily transformed to 12 by iodization, and the iodine atom of 12 was converted to a C-C or C-N bond by means of palladium-catalyzed reaction to afford 13. Transcriptional activation assay revealed that 13g (in which the iodine atom was replaced with an amino group) is a weak RXR agonist, while 13d (a phenyl group), 13e (a styryl group), and 13f (an anilino group) are RXR antagonists. Among them, 13e was found to be more potent than the known RXR antagonist PA452 (9).

Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's oligomeric switch.[Pubmed:20188110]

J Mol Biol. 2010 Apr 16;397(5):1121-31.

Ligands that activate the nuclear receptor retinoid X receptor (RXR) display potent anticarcinogenic activities, but the mechanisms by which these compounds inhibit carcinoma cell growth are poorly understood. While RXR can regulate gene expression due to its intrinsic ligand-activated transcription function, this receptor can also regulate transcription by functioning as a ligand-controlled DNA architectural factor. It was thus reported that apo-RXR self-associates into tetramers and that each dimer within these tetramers can separately bind to an RXR response element. Hence, DNA binding by RXR tetramers may bring distant genomic regions into close physical proximity. As ligand binding induces the dissociation of RXR tetramers into dimers, it can alter gene expression by modulating the DNA architecture. Here, we show that inhibition of mammary carcinoma cell growth by RXR ligands stems from the ability of these compounds to regulate the oligomeric state of RXR and is independent of the direct intrinsic transcriptional activity of the receptor. The data suggest that compounds that trigger dissociation of RXR tetramers may comprise a novel class of anticarcinogenic agents.

Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.[Pubmed:12139443]

J Med Chem. 2002 Aug 1;45(16):3327-30.

Several 2-(arylamino)pyrimidine-5-carboxylic acids were designed as novel retinoid X receptor (RXR) antagonists. Compound 6a or 6b alone did not exhibit differentiation-inducing activity toward HL-60 cells and did not affect the activity of a retinoic acid receptor (RAR) agonist, Am80, but did inhibit the synergistic activity of an RXR agonist, PA024 (3), in the presence of Am80. The activity of 6 was ascribed to selective antagonism at the RXR site of RXR-RAR heterodimers.

Description

PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.

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