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
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
CGP 52608, ≥98%, solid
方案
≥98%
表单
solid
溶解性
DMSO: >30 mg/mL
H2O: insoluble
储存温度
−20°C
SMILES字符串
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
相关类别
应用
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.
生化/生理作用
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.
特点和优势
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
I Wiesenberg et al.
Molecular pharmacology, 53(6), 1131-1138 (1998-06-17)
The thiazolidinedione BRL 49653 and the thiazolidinedione derivative CGP 52608 are lead compounds of two pharmacologically different classes of compounds. BRL 49653 is a high affinity ligand of peroxisome proliferator-activated receptor gamma (PPARgamma) and a prototype of novel antidiabetic agents
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
Cagri Gulec et al.
Experimental cell research, 353(1), 6-15 (2017-02-28)
ROR-alpha is a nuclear receptor, activity of which can be modulated by natural or synthetic ligands. Due to its possible involvement in, and potential therapeutic target for atherosclerosis, we aimed to identify ROR-alpha target genes in monocytic and endothelial cell
J E Roberts et al.
Journal of pineal research, 29(2), 94-99 (2000-09-12)
Previous work has demonstrated that melatonin inhibits the growth of both dermal and uveal melanoma cells. Recent clinical trials have found that melatonin is an efficacious treatment for metastatic dermal melanoma. The goal of this study was to provide further
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
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