Glyoxylase I (GloΙ) Inhibitor COTC
Date:July 07 2021Web Page No:95016
2-Crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxycyclohex-2-enone (COTC) is an inhibitor of glyoxylase I isolated from the culture of Streptomyces griseosporeus MD287-CF3 1, 2).
COTC shows a strong growth inhibition of HeLa cells and Ehrlich ascites carcinoma with low toxicity (LD50 mice:90 mg/kg i.v.) 1). COTC reacts with glutathione or other SH-compounds to form corresponding thioethers 2, 4). Synthesis of COTC derivatives for antitumor activity has also been reported 6).
6-epi-COTC, one of the diastereomers of COTC and COMC, a synthetic analog of COTC with a simplified structure are also available.
Specification
CAS# | 57449-30-6 |
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Molecular Formula | C11H14O6 |
Molecular Weight | 242.227 |
Source | Streptomyces griseosporeus MD287-CF3 |
Purity | >98% (HPLC) |
Solubility | Soluble in MeOH, DMSO and H2O Insoluble in n-Hexane |
Application Note
- OCTC shows IC50 values against rat liver crude glyoxalase and yeast glyoxalase I at 1.8 mM and 1.4 mM, respectively, in a reaction mixture containing 1.59 mM of reduced glutathione and preincubated for 3 minutes before enzyme addition 1, 3).
- COTC blocks enzymatic activity of alkaline phosphodiesterase derived from murine lymphoblastoma L5178Y cells (IC50: 60 μg/ml). COTC and aclarubicin exhibits synergistic activity on aclarubicin-resistant cells, but not on the parental cells 5).
Reference
- Takeuchi T., et al., J. Antibiot., 28 (10), 737~742 (1975). [PMID:1102510]
- Chimura H., et al., J. Antibiot., 28 (10), 743~748 (1975). [PMID:1184466]
- Matsuda A., et al., Japanese Patent, JPS52113946A (1977).
- Huntley C.F., et al., Org. Lett., 2 (20), 3,143~3,144 (2000). [PMID:11009366]
- Sugimoto Y., et al., J. Antibiot., 35 (9), 1,222~1,230 (1982). [PMID:7142023]
- Tony K.M.S., et al., Bioorg. Med. Chem. Lett., 22 (24), 7,562~7,565 (2012). [PMID:23102892]
[Date : November 02 2024 00:08]
Detail | Product Name | Product Code | Supplier | Size | Price | ||||||||||||||||||||||||||||||
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COTC, Glyoxalase-I Inhibitor DatasheetThis may not be the latest data sheet. |
14675 | IMCInstitute of Microbial Chemistry | 1 mg | $500 | |||||||||||||||||||||||||||||||
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[Date : November 02 2024 00:08]
COTC, Glyoxalase-I Inhibitor
DatasheetThis may not be the latest data sheet.
- Product Code: 14675
- Supplier: IMC
- Size: 1mg
- Price: $500
Description | |||
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Storage | -20°C | CAS | 57449-30-6 |
Link |
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