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经验公式(希尔记法):
C8H12N4OS2
化学文摘社编号:
分子量:
244.34
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
CGP 52608, ≥98%, solid
SMILES string
CNC(=S)N\N=C1/SCC(=O)N1CC=C
InChI key
DDYJDIHOSRTMSE-FLIBITNWSA-N
InChI
1S/C8H12N4OS2/c1-3-4-12-6(13)5-15-8(12)11-10-7(14)9-2/h3H,1,4-5H2,2H3,(H2,9,10,14)/b11-8-
assay
≥98%
form
solid
solubility
DMSO: >30 mg/mL, H2O: insoluble
storage temp.
−20°C
Quality Level
Application
CGP 52608 has been used as a RAR related orphan receptor α (RORα) synthetic agonist in THP-1 macrophages, in human monocyte cells THP1 and somatic testicular cells.
Biochem/physiol Actions
CGP 52608 is a specific activator of retinoic acid receptor-related orphan receptor α (RORA).
CGP 52608 is a thiazolidine derivative and an antiarthritic compound. It possesses immunostimulatory functionality and elicits antiproliferative effect in colon tumors. It is cytotoxic towards neural cell lines. CGP 52608 induces apoptosis in tumor and also favors G0-G1 cell cycle phase accumulation in neural cell lines.
Features and Benefits
This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Katarzyna Winczyk et al.
Neuro endocrinology letters, 27(3), 351-354 (2006-07-04)
Melatonin may influence directly tumor cells through the specific binding sites. The best known melatonin binding sites are membrane receptors. Recently, the participation of nuclear signalling via estrogen as well as RZR/ROR receptors in oncostatic action of melatonin on the
Mercedes M Leon-Blanco et al.
Cancer letters, 216(1), 73-80 (2004-10-27)
The RNA expression levels of human catalytic subunit (TERT) and the RNA subunit (TR) of telomerase were analysed after treatment with the agonists of the membrane receptor (S 20098) and the nuclear receptor (CGP 52608) for melatonin in the MCF-7
M Missbach et al.
The Journal of biological chemistry, 271(23), 13515-13522 (1996-06-07)
Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead
R M Moretti et al.
International journal of cancer, 92(5), 733-737 (2001-05-08)
Thiazolidinedione derivatives with potent antiarthritic activity, such as CGP 52608, have been suggested to exert their biological effects through the activation of the orphan nuclear receptor RORalpha. Since response elements for this receptor are present in the promoter region of
R M Moretti et al.
The Prostate, 46(4), 327-335 (2001-03-10)
RORalpha is a transcription factor which belongs to the family of orphan nuclear receptors. The regulatory functions of this receptor are still poorly understood. However, response elements for RORalpha are present on the promoter of cell cycle-related genes suggesting that
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