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
Quality Level
assay
≥98%
form
solid
solubility
DMSO: >30 mg/mL, H2O: insoluble
storage temp.
−20°C
SMILES string
CNC(=S)N\N=C1/SCC(=O)N1CC=C
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-
InChI key
DDYJDIHOSRTMSE-FLIBITNWSA-N
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
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
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
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
Andrea Balla et al.
Neuropharmacology, 56(5), 915-921 (2009-04-18)
Deficits in N-methyl-D-aspartate receptor (NMDAR)-mediated neurotransmission may underlie dopaminergic hyperactivity in schizophrenia. Dysregulation of the GABAergic system has also been implicated. In this study we investigated a role for GABA(B) receptors as an intermediate step in the pathway leading from
P T Ram et al.
Cancer letters, 179(2), 141-150 (2002-03-13)
Two putative melatonin receptors have been described including the cell surface G-protein-linked receptors, mt1 and MT2, and the nuclear retinoic orphan receptor alpha (RORalpha). The mt1 receptor, but not the MT2 receptor, is expressed in human breast tumor cell lines
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We offer many products related to non-steroid nuclear receptors for your research needs.
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| C5749-5MG | 04061832954172 |
| C5749-25MG | 04061832954165 |
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