中文同义词:
GAMMA-SECRETASE抑制剂(Z-ILE-LEU-ALDEHYDE)
英文名称:
GAMMA-SECRETASE INHIBITOR XII
英文同义词:
Z-ILE-LEU-ALDEHYDE;Z-IL-CHO;GAMMA-SECRETASE INHIBITOR XII;γ-Secretase inhibitor XII (GSI-XII);GSI-XII);Z-Ile-Leu-aldehyde(Z-IL-CHO;Z-ILE-LEU-ALDEHYDE(Z-IL-CHO; GSI-XII);Z-IL-CHO;GSI-XII;Γ-SECRETASE INHIBITOR XII
沸点
545.6±45.0 °C(Predicted)
密度
1.074±0.06 g/cm3(Predicted)
酸度系数(pKa)
11.14±0.46(Predicted)
生物活性
Z-Ile-Leu-aldehyde (Z-IL-CHO) 是有效的、竞争性的 γ-secretase 和 notch 的肽醛抑制剂。
体外研究
Z-Ile-Leu-aldehyde (ILCHO) significantly downregulates Th17-associated cytokine levels in murine Th17 in vitro polarization assays.
Z-Ile-Leu-aldehyde (GSI XII) induces apoptosis of murine MOPC315.BM myeloma cells with high Notch activity.
RT-PCRsup>[1]
Cell Line: CD4 + T cells from C57BL/6 mice.
Concentration: 25 μM.
Incubation Time: 24, 48, 72 hours.
Result: DownregulateD RORt and IL-17 mRNA expression.
Cell Viability Assaysup>[2]
Cell Line: MOPC315.BM cells.
Concentration: 0, 12, 15 μM.
Incubation Time: 24-48 h hours.
Result: Reduced viability and induced apoptosis in MOPC315.BM cells
Cell Line:
CD4 + T cells from C57BL/6 mice.
Incubation Time:
24, 48, 72 hours.
Result:
DownregulateD RORt and IL-17 mRNA expression.
Cell Line:
MOPC315.BM cells.
Concentration:
0, 12, 15 μM.
Incubation Time:
24-48 h hours.
Result:
Reduced viability and induced apoptosis in MOPC315.BM cells
体内研究
Z-Ile-Leu-aldehyde (GSI XII, 10 mg/kg, Intraperitoneally either for 14 days) controls myeloma bone disease mainly by targeting Notch in MM cells and possibly in osteoclasts in their microenvironment.
Animal Model: MOPC315.BM mouse model.
Dosage: 10 mg/kg.
Administration: Intraperitoneally either for 14 days.
Result: Reduces myeloma-specific paraprotein levels in the MOPC315.BM model.
Diminished osteolytic lesions in the MOPC315.BM mice.
Animal Model:
MOPC315.BM mouse model.
Administration:
Intraperitoneally either for 14 days.
Result:
Reduces myeloma-specific paraprotein levels in the MOPC315.BM model.
Diminished osteolytic lesions in the MOPC315.BM mice.
