O8890
OU749
≥98% (HPLC)
Synonym(s):
N-[5-(4-Methoxybenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
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About This Item
Empirical Formula (Hill Notation):
C16H15N3O3S2
CAS Number:
Molecular Weight:
361.44
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
InChI
1S/C16H15N3O3S2/c1-22-13-9-7-12(8-10-13)11-15-17-18-16(23-15)19-24(20,21)14-5-3-2-4-6-14/h2-10H,11H2,1H3,(H,18,19)
SMILES string
COc1ccc(Cc2nnc(NS(=O)(=O)c3ccccc3)s2)cc1
InChI key
QCXWBMZVLJCKHF-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
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.
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).
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Xinlei Yu et al.
Scientific reports, 6, 30033-30033 (2016-07-19)
Although essential amino acids regulate mechanistic target of rapamycin complex 1 (mTORC1) and the integrated stress response (ISR), the role of cysteine is unknown. We found that in hepatoma HepG2 cells, cystine (oxidized form of cysteine) activated mTORC1 and suppressed
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