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Submit ReviewHX 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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 9.67 | 20 |
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 |
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.
Keywords: HX 531, HX 531 supplier, HX531, rxrs, retinoids, x, receptors, antagonists, potent, stem, cell, differentiation, adipocytes, Retinoid, X, Receptor, 3912, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for HX 531 include:
Adriano et al (2018) Toward Minimal Residual Disease-Directed Therapy in Melanoma. Cell 174 843-855.e19 PMID: 30017245
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
Wnuk et al (2016) The Crucial Involvement of Retinoid X Receptors in DDE Neurotoxicity. PLoS Biol 29 155 PMID: 26563996
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
Nie et al (2017) Brown adipogenic reprogramming induced by a small molecule. Cell.Rep. 18 624 PMID: 28099842
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
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
Edwards et al (2019) Assessment of total, ligand-induced peroxisome proliferator activated receptor γ ligand activity in serum. Environ Health 18 45 PMID: 31072366
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
Rui et al (2020) Phenotypic landscape of intestinal organoid regeneration. Nature 586 275-280 PMID: 33029001
Ane et al (2021) Retinoic acid signaling is critical during the totipotency window in early mammalian development. Nat Struct Mol Biol 28 521-532 PMID: 34045724
Do you know of a great paper that uses HX 531 from Tocris? Please let us know.
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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