化驗
≥98% (HPLC)
形狀
powder
顏色
white to off-white
溶解度
DMSO: >20 mg/mL
儲存溫度
2-8°C
SMILES 字串
COc1ccc(Cc2nnc(NS(=O)(=O)c3ccccc3)s2)cc1
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)
InChI 密鑰
QCXWBMZVLJCKHF-UHFFFAOYSA-N
生化／生理作用
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).
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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