HX 531

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Cat.No. 3912 - HX 531 | C29H29N3O4 | CAS No. 188844-34-0
Description: Potent RXR antagonist
Chemical Name: 4-(7,8,9,10-Tetrahydro-5,7,7,10.10-pentamethyl-2-nitro-5H-benzo[b]naphtho[2,3-e][1,4]-diazepin-12-yl)-benzoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews (1)
Literature (3)

Biological Activity

Potent RXR antagonist (IC50 = 18 nM). Promotes white and brown pre-adipocyte differentiation into white adipocytes. Also inhibits bexarotene-induced brown adipogenic reprogramming of myoblasts.

Technical Data

M. Wt 483.56
Formula C29H29N3O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 188844-34-0
PubChem ID 11755040
InChI Key SXKPGYKPQPYJER-UHFFFAOYSA-N
Smiles CC1(C)C2=C(C=C(N(C)C(C=CC([N+]([O-])=O)=C5)=C5N=C3C4=CC=C(C(O)=O)C=C4)C3=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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 9.67 20

Preparing Stock Solutions

The following data is based on the product molecular weight 483.56. 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
0.2 mM 10.34 mL 51.7 mL 103.4 mL
1 mM 2.07 mL 10.34 mL 20.68 mL
2 mM 1.03 mL 5.17 mL 10.34 mL
10 mM 0.21 mL 1.03 mL 2.07 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Ebisawa et al (1999) Retinoid X receptor-antagonistic diazepinylbenzoic acids. Chem.Pharm.Bull. 47 1778 PMID: 10748721

Alique et al (2006) Vitamin A active metabolite, all-trans retinoic acid, induces spinal cord sensitization. II. Effects after intrathecal administration. Br.J.Pharmacol. 149 65 PMID: 16847438

Suzuki et al (2009) Docosahexaenoic acid induces adipose differentiation-related protein through activation of retinoid X receptor in human choriocarcinoma BeWo cells. Biol.Pharm.Bull. 32 1177 PMID: 19571381

Nie et al (2017) Brown adipogenic reprogramming induced by a small molecule. Cell Rep. 18 624 PMID: 28099842


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Keywords: HX 531, HX 531 supplier, HX531, rxrs, retinoids, x, receptors, antagonists, potent, stem, cell, differentiation, adipocytes, Retinoid, X, Receptor, 3912, Tocris Bioscience

7 Citations for HX 531

Citations are publications that use Tocris products. Selected citations for HX 531 include:

Wnuk et al (2017) Benzophenone-3 Impairs Autophagy, Alters Epigenetic Status, and Disrupts Retinoid X Receptor Signaling in Apoptotic Neuronal Cells. Mol Neurobiol PMID: 28815487

Cherian et al (2015) CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol Pharmacol 87 878 PMID: 25762023

Nie et al (2017) Brown adipogenic reprogramming induced by a small molecule. Cell.Rep. 18 624 PMID: 28099842

Edwards et al (2019) Assessment of total, ligand-induced peroxisome proliferator activated receptor γ ligand activity in serum. Environ Health 18 45 PMID: 31072366

Yang et al (2017) Effects of electroacupuncture and the retinoid X receptor (RXR) signalling pathway on oligodendrocyte differentiation in the demyelinated spinal cord of rats. Acupunct Med 35 122 PMID: 27841975

Wnuk et al (2016) The Crucial Involvement of Retinoid X Receptors in DDE Neurotoxicity. PLoS Biol 29 155 PMID: 26563996

Summermatter et al (2013) Skeletal muscle PGC-1α controls whole-body lactate homeostasis through estrogen-related receptor α-dependent activation of LDH B and repression of LDH A. Proc Natl Acad Sci U S A 110 8738 PMID: 23650363


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Reviews for HX 531

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Complete ablation of RA-induced transcription in MCF7.
By Anonymous on 11/02/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: MCF7

HX531 was dissolved to a concentration of 20 mM in DMSO with no solubility issues. Retinoic acid (10 uM), DMSO, or RA + HX531 (1 uM) was added to MCF7 cells for 5 hours following by qPCR analysis of a reporter gene normalized to GAPDH levels. 1 uM of HX531 completely ablated RA induced gene transcription by qPCR. This inhibitor exhibited lower variability than AGN193109, however this was repeated only once, and both inhibitors could completely ablate activity, either alone or in combination. We also added retinal to confirm that our reporter activity was retinoic acid-specific.

No apoptosis has been observed in any of our cells lines at 1 uM

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Literature in this Area

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