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Submit ReviewHX 531
说明： Potent RXR antagonist
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for HX 531
| 分子量 | 483.56 |
| 公式 | C29H29N3O4 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for HX 531
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 9.67 | 20 |
制备储备液 for HX 531
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for HX 531
参考文献 for HX 531
参考文献是支持产品生物活性的出版物。
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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关键词: HX 531, HX 531 supplier, HX531, rxrs, retinoids, x, receptors, antagonists, potent, stem, cell, differentiation, adipocytes, Retinoid, X, Receptor, 3912, Tocris Bioscience
12 篇 HX 531 的引用文献
引用文献是使用了 Tocris 产品的出版物。 HX 531 的部分引用包括：
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
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HX 531 的评论
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Complete ablation of RA-induced transcription in MCF7.
By
Anonymous on 11/02/2019
分析类型： In Vitro
种属： Human
细胞系/组织： 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
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.