HX 630

RXR synergist CAS# 188844-52-2

HX 630

2D Structure

Catalog No. BCC6083----Order now to get a substantial discount!

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HX 630: 5mg $138 In Stock
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3D structure

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HX 630

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Chemical Properties of HX 630

Cas No. 188844-52-2 SDF Download SDF
PubChem ID 9889522 Appearance Powder
Formula C28H27NO2S M.Wt 441.58
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 4-(7,7,10,10-tetramethyl-8,9-dihydronaphtho[2,3-b][1,5]benzothiazepin-12-yl)benzoic acid
SMILES CC1(CCC(C2=C1C=C3C(=C2)SC4=CC=CC=C4N=C3C5=CC=C(C=C5)C(=O)O)(C)C)C
Standard InChIKey PFGCWQPTOKPRRK-UHFFFAOYSA-N
Standard InChI InChI=1S/C28H27NO2S/c1-27(2)13-14-28(3,4)21-16-24-19(15-20(21)27)25(17-9-11-18(12-10-17)26(30)31)29-22-7-5-6-8-23(22)32-24/h5-12,15-16H,13-14H2,1-4H3,(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 HX 630

DescriptionRXR agonist. Acts as a retinoid synergist; enhances the potency of AM 80 in a HL-60 cell differentiation assay.

HX 630 Dilution Calculator

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Preparing Stock Solutions of HX 630

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2646 mL 11.323 mL 22.646 mL 45.2919 mL 56.6149 mL
5 mM 0.4529 mL 2.2646 mL 4.5292 mL 9.0584 mL 11.323 mL
10 mM 0.2265 mL 1.1323 mL 2.2646 mL 4.5292 mL 5.6615 mL
50 mM 0.0453 mL 0.2265 mL 0.4529 mL 0.9058 mL 1.1323 mL
100 mM 0.0226 mL 0.1132 mL 0.2265 mL 0.4529 mL 0.5661 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 HX 630

Clinically potential subclasses of retinoid synergists revealed by gene expression profiling.[Pubmed:12533672]

Mol Cancer Ther. 2003 Jan;2(1):49-58.

Retinoids have chemopreventive and therapeutic potency in oncology and dermatology, although their application is restricted by many undesirable side effects. For the development of more effective and less toxic retinoids, gene expression analyses using DNA microarrays have the potential to supplement conventional screening methods, which are based on the changes in cell morphology and/or function. In this study, we applied the class prediction algorithm, which was used in the molecular phenotyping of tumors, for the classification of synthetic retinoids (Am80 and Tp80) and retinoid synergists (HX630, TZ335, and PA024) as all-trans retinoic acid-like, 9-cis retinoic acid-like, and control-like classes. By analyzing the effects of all-trans retinoic acid and 9-cis retinoic acid on the gene expressions in a human promyelocytic leukemia cell line, HL60, we successfully selected 50 marker genes whose expression pattern could distinguish these classes. Moreover, the classification revealed the existence of two subclasses among the retinoid synergists used with Am80. Close inspection of the DNA microarray analyses indicated that these two subclasses had different effects on the apoptosis of HL60 cells, and this was confirmed by in vivo experiments. These results indicate that the retinoidal activity of Am80, which has already been used in clinical trials, could be modulated differently by the two classes of retinoid synergists. Thus, these two subclasses of retinoid synergists have the potency to widen the usage of Am80. Our analyses demonstrated that the gene expression profiling could provide important information for developing useful retinoid synergists by compensating conventional screening methods.

Effect of natural and synthetic retinoids on the proliferation and differentiation of three canine melanoma cell lines.[Pubmed:11913557]

J Vet Med Sci. 2002 Feb;64(2):169-72.

The effect of two natural retinoids and synthetic retinoids with or without retinoid synergists on the proliferation and differentiation of 3 melanoma cell lines were investigated in vitro. No retinoids showed significant growth inhibitory effect on these cell lines when used alone, however, cell differentiation and significant growth inhibition were observed when treated with a combination of retinoids and a retinoid synergist. This study may suggest that, though the cells showed low susceptibilities when retinoids were treated alone, the combination of retinoids and a retinoid synergist may be effective to control the growth of canine melanoma cell lines.

Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.[Pubmed:9435893]

J Med Chem. 1997 Dec 19;40(26):4222-34.

In human HL-60 promyelocytic leukemia cells, diazepinylbenzoic acid derivatives can exhibit either antagonistic or synergistic effects on the differentiation-inducing activities of natural or synthetic retinoids, the activity depending largely on the nature of the substituents on the diazepine ring. Thus, a benzolog of the retinoid antagonist LE135 (6), 4-(13H-10,11,12,13-tetrahydro-10, 10,13,13,15-pentamethyldinaphtho[2,3-b][1,2-e]diazepin-7-yl) benzoic acid (LE540, 17), exhibits a 1 order of magnitude higher antagonistic potential than the parental LE135 (6). In contrast, 4-[5H-2,3-(2,5-dimethyl-2,5-hexano)-5-methyldibenzo[b,e] [1,4]diazepin-11-yl]-benzoic acid (HX600, 7), a structural isomer of the antagonistic LE135 (6), enhanced HL-60 cell differentiation induced by RAR agonists, such as Am80 (2). This synergistic effect was further increased for a thiazepine, HX630 (29), and an azepine derivative, HX640 (30); both synergized with Am80 (2) more potently than HX600 (7). Notably, the negative and positive effects of the azepine derivatives on retinoidal actions can be related to their RAR-antagonistic and RXR-agonistic properties, respectively, in the context of the RAR-RXR heterodimer.

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