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C5749
CGP 52608
≥98%, solid
Synonym(s):
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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5 MG
€155.00
25 MG
€574.00
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5 MG
€155.00
25 MG
€574.00
About This Item
Empirical Formula (Hill Notation):
C8H12N4OS2
CAS Number:
Molecular Weight:
244.34
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Recommended Products
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
Biochem/physiol Actions
CGP 52608 is a specific activator of retinoic acid receptor-related orphan receptor α (RORA).
CGP 52608 is a thiazolidine derivative[4] and an antiarthritic compound.[5] It possesses immunostimulatory functionality[4] and elicits antiproliferative effect in colon tumors.[6] It is cytotoxic towards neural cell lines.[5] CGP 52608 induces apoptosis in tumor[6] and also favors G0-G1 cell cycle phase accumulation in neural cell lines.[5]
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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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
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
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
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
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
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