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CD 437 (Synonyms: CD437)

Catalog No.GC11464

RARγ-selective agonist,potent and cell-permeable

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CD 437 Chemical Structure

Cas No.: 125316-60-1

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10mM (in 1mL DMSO)
$67.00
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5mg
$47.00
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10mg
$68.00
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50mg
$272.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

For morphological analysis, cells are treated with 10 μM CD437, trypsinized, washed with phosphate-buffered saline (PBS), fixed with 3.7% paraformaldehyde, and stained with 50 μg of 4,6-diamidino-2-phenylindole (DAPI) per mL containing 100 μg of DNase-free RNase A per mL to visualize the nuclei. Stained cells are examined by fluorescence microscopy. For the terminal deoxynucleotidyl transferase (TdT) assay, cells are treated with or without 10 μM CD437. After treatment, cells are trypsinized, washed with PBS, fixed in 1% formaldehyde in PBS, washed with PBS, resuspended in 70% ice-cold ethanol, and immediately stored at -20°C overnight. Cells are then labeled with biotin-16-dUTP by terminal transferase and stained with avidin-FITC (fluorescein isothiocyanate). The labeled cells are analyzed with a flow cytometer[1].

Animal experiment:

Male Swiss-nu/nu mice weighing 20 to 25 g are used in this study. Mice are kept under sterile conditions at 24 to 26°C room temperature, 50% relative humidity, and 12 h light-dark rhythm in laminar flow shelves and are supplied with autoclaved food and bedding. For treatment of melanoma xenografts, previously established MeWo melanoma tumors of 1 to 2 mm in diameter are implanted into the right flank of animals. After tumor growth for 10 d, groups of mice (n=8) are either treated with saline p.o. or are injected intratumorally for 3 wk or are fed with various concentrations of CD437 (10 mg/kg/body weight and 30 mg/kg/body weight). In addition, tumors of a fifth group are injected with CD437 (10 mg/kg/body weight) each day. Mice are visited daily and growing tumors are measured twice weekly with a caliperlike instrument[2].

References:

[1]. Li Y, et al. Molecular determinants of AHPN (CD437)-induced growth arrest and apoptosis in human lung cancer cell lines. Mol Cell Biol. 1998 Aug;18(8):4719-31.
[2]. Schadendorf D, et al. Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo. J Cell Biol. 1996 Dec;135(6 Pt 2):1889-98.

Background

CD 437 is a selective agonist of RARγ [1].

Retinoic acid receptor gamma (RAR-γ) is a nuclear receptor that is activated by 9-cis retinoic acid and all-trans retinoic acid. RAR-γ also functions as a transcription factor.

CD 437 is a selective RARγ agonist. In tumor cells, CD437 induced RAR-γ-dependent differentiation and apoptosis. Also, CD437 induced DNA adduct formation and p53-independent DNA damage response [1]. In DU145 human prostate cancer cells, CD437 rapidly reduced IκBα and increased nuclear translocation of the NF-κB subunit p65. Also, CD437 increased the DNA-binding activity of NF-κB and induced DR4 expression and apoptosis [2]. In human melanoma A375 cells, CD437 induced apoptosis, which was mediated by the activation of NF-κB and RIG-I (retinoic acid inducible gene I) pathway [3]. In human osteosarcoma cells, CD437 activated c-Jun N-terminal kinase 1 (JNK1) through the upregulation of thioredoxin-binding protein 2 (TBP2) and induced apoptosis. Also, CD437 induced TBP2 mRNA expression by recruitment of ETS1 transcription factor [4].

References:
[1].  Zhao X, Spanjaard RA. The apoptotic action of the retinoid CD437/AHPN: diverse effects, common basis. J Biomed Sci, 2003, 10(1): 44-49.
[2].  Jin F, Liu X, Zhou Z, et al. Activation of nuclear factor-kappaB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res, 2005, 65(14): 6354-6363.
[3].  Pan M, Geng S, Xiao S, et al. Apoptosis induced by synthetic retinoic acid CD437 on human melanoma A375 cells involves RIG-I pathway. Arch Dermatol Res, 2009, 301(1): 15-20.
[4].  Hashiguchi K, Tsuchiya H, Tomita A, et al. Involvement of ETS1 in thioredoxin-binding protein 2 transcription induced by a synthetic retinoid CD437 in human osteosarcoma cells. Biochem Biophys Res Commun, 2010, 391(1): 621-626.

Chemical Properties

Cas No. 125316-60-1 SDF
Synonyms CD437
Chemical Name 6-(3-((1s,3R,5S,7s)-adamantan-1-yl)-4-hydroxyphenyl)-2-naphthoic acid
Canonical SMILES OC1=CC=C(C2=CC=C3C(C=CC(C(O)=O)=C3)=C2)C=C1[C@]4(C[C@@H]5C6)C[C@@H]6C[C@H](C5)C4
Formula C27H26O3 M.Wt 398.5
Solubility DMF: 10 mg/ml,DMSO: 16 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.05 mg/ml,Ethanol: 1 mg/ml Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5094 mL 12.5471 mL 25.0941 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 mL
10 mM 0.2509 mL 1.2547 mL 2.5094 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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