HX 531

Pricing Availability   Qty
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)
Citations (12)
Reviews (1)
Literature (1)

Biological Activity for HX 531

HX 531 is a 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 for HX 531

M. Wt 483.56
Formula C29H29N3O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 188844-34-0
PubChem ID 11755040
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 for HX 531

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

Preparing Stock Solutions for HX 531

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.

Select a batch to recalculate based on the batch molecular weight:
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 for HX 531

Certificate of Analysis / Product Datasheet
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References for HX 531

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

If you know of a relevant reference for HX 531, please let us know.

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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

12 Citations for HX 531

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

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

Olle et al (2017) Testicular organoid generation by a novel in vitro three-layer gradient system. Biomaterials 130 76-89 PMID: 28364632

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

Karen T et al (2020) The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer. Sci Rep 10 22244 PMID: 33335263

Do you know of a great paper that uses HX 531 from Tocris? Please let us know.

Reviews for HX 531

Average Rating: 5 (Based on 1 Review.)

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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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Retinoid Receptors Scientific Review

Retinoid Receptors Scientific Review

Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.