C5749
CGP 52608
≥98%, RORA activator, solid
别名:
1-[3-Allyl-4-oxo-thiazolidine-2-ylidene]-4-methyl-thiosemicarbazone, N-Methyl-2-[4-oxo-3-(2-propen-1-yl)-2-thiazolidinylidene]-hydrazinecarbothioamide
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关于此项目
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
K Winczyk et al.
Journal of pineal research, 31(2), 179-182 (2001-09-14)
The effects of melatonin and the thiazolinidinedione derivative CGP 52608 on apoptosis of Colon 38 cancer cells were investigated. Male mice were implanted subcutaneously with a suspension of Colon 38 cells. Ten days after induction of tumors, the animals were
Michal Karasek et al.
Journal of pineal research, 34(4), 294-296 (2003-03-29)
Melatonin exerts a marked antiproliferative action in numerous experimentally-induced tumors in vivo as well as in both animal and human cell lines in vitro. However, the mechanisms of oncostatic action of melatonin is not clear, and the involvement of both
Shou-Long Deng et al.
Oncotarget, 8(66), 110592-110605 (2018-01-05)
Because androgen function is regulated by its receptors, androgen-androgen receptor signaling is crucial for regulating spermatogenesis. Androgen is mainly testosterone secreted by testis. Based on the results of early studies in goats, the administration of melatonin over an extended period
J E Roberts et al.
Journal of pineal research, 28(3), 165-171 (2000-03-30)
Previous work has demonstrated that melatonin inhibits growth of cultured human uveal melanoma cells. The goal of this study was to determine the expression of mRNA encoding the melatonin receptor subtypes and the effect of specific melatonin receptor agonists on
M Karasek et al.
Biological signals and receptors, 8(1-2), 75-78 (1999-03-23)
The antiproliferative effects of melatonin and CGP 52608, an exogenous ligand for RZR/ROR receptors, are compared in the present paper. Both compounds exerted similar inhibitory effects on the proliferation of neoplastic cells in mouse colonic adenocarcinoma, DU 145 human prostate
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