Z-ILE-LEU-ALDEHYDE

中文名称:

Z-ILE-LEU-ALDEHYDE

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

CAS号:

161710-10-7

分子式:

C20H30N2O4

分子量:

362.46

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

161710-10-7.mol

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 RORt 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.

Concentration:

25 μM.

Incubation Time:

24, 48, 72 hours.

Result:

DownregulateD RORt 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.

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.