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C5749

CGP 52608

Name: CGP 52608
Brand: SIGMA

≥98%, RORA activator, 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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About This Item

Empirical Formula (Hill Notation):

C₈H₁₂N₄OS₂

CAS Number:

87958-67-6

Molecular Weight:

244.34

UNSPSC Code:

12352200

PubChem Substance ID:

329775098

NACRES:

NA.77

MDL number:

MFCD00942304

Assay:

≥98%

Form:

solid

Quality level:

100

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Product Name

CGP 52608, ≥98%, solid

Quality Level

100

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

Related Categories

Bioactive Small Molecules

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Growth-inhibitory action of melatonin and thiazolidinedione derivative CGP 52608 on murine 16/C breast cancer cells.

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

RNA expression of human telomerase subunits TR and TERT is differentially affected by melatonin receptor agonists in the MCF-7 tumor cell line.

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

Thiazolidine diones, specific ligands of the nuclear receptor retinoid Z receptor/retinoid acid receptor-related orphan receptor alpha with potent antiarthritic activity.

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

Photophysical studies on melatonin and its receptor agonists.

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

Specific activation of the nuclear receptors PPARgamma and RORA by the antidiabetic thiazolidinedione BRL 49653 and the antiarthritic thiazolidinedione derivative CGP 52608.

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

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Nuclear Receptors (Non-Steroids)

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Global Trade Item Number

SKU	GTIN
C5749-5MG	04061832954172
C5749-25MG	04061832954165

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