OU749

• Catalog No.: O8890
• CAS Number: 519170-13-9
• M. F.: C16H15N3O3S2
• M. W.: 361.4386
• Purity: ≥98% (HPLC)

SYNONYMS

• IUPAC name: N-{5-[(4-methoxyphenyl)methyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide
• IUPAC Traditional name: N-{5-[(4-methoxyphenyl)methyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide
• Synonyms: N-[5-(4-Methoxybenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide

DATABASE IDS

• CAS Number: 519170-13-9
• MDL Number: MFCD03351667

PROPERTIES

• Empirical Formula (Hill Notation): C16H15N3O3S2
• Purity: ≥98% (HPLC)
• Apperance: white to off-white powder
• Solubility: DMSO: >20 mg/mL
• GHS Signal Word: Warning
• GHS Hazard statements: H302
• European Hazard Symbols: Harmful (Xn)
• Risk Statements: 22
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

Biochem/physiol Actions
Gamma-glutamyl transpeptidase (GGT; aka gamma-glutamyl transferase) cleaves the gamma-glutamyl bond of glutathione, making extracellular glutathione available for intracellular use. Elevated intracellular glutathione contributes to resistance of tumors to chemotherapy and radiation. GGT is a therapeutic target for treatment-resistance cancers, as treatment with GGT inhibitors prior to chemotherapy or radiation could sensitize GGT-positive tumors to treatment by decreasing glutathione levels. Previously, all GGT inhibitors have been glutamine analogues, which are competitive for the gamma-glutamyl site. Due to high toxicity, these compounds cannot be used in the clinic. OU749 is the first non-glutamine GGT inhibitor. It is also non-competitive for the gamma-glutamyl site. OU749 inhibits human GGT in an enzyme assay and is much less toxic than other GGT inhibitors, including azaserine (glutamine analogue, Sigma catalog).

Description (简体中文)

Biochem/physiol Actions
Gamma-glutamyl transpeptidase (GGT; aka gamma-glutamyl transferase) cleaves the gamma-glutamyl bond of glutathione, making extracellular glutathione available for intracellular use. Elevated intracellular glutathione contributes to resistance of tumors to chemotherapy and radiation. GGT is a therapeutic target for treatment-resistance cancers, as treatment with GGT inhibitors prior to chemotherapy or radiation could sensitize GGT-positive tumors to treatment by decreasing glutathione levels. Previously, all GGT inhibitors have been glutamine analogues, which are competitive for the gamma-glutamyl site. Due to high toxicity, these compounds cannot be used in the clinic. OU749 is the first non-glutamine GGT inhibitor. It is also non-competitive for the gamma-glutamyl site. OU749 inhibits human GGT in an enzyme assay and is much less toxic than other GGT inhibitors, including azaserine (glutamine analogue, Sigma catalog).