Z-ILE-LEU-ALDEHYDE

生物活性体外研究体内研究 Z-ILE-LEU-ALDEHYDE 试剂级价格

Z-ILE-LEU-ALDEHYDE

CAS号:161710-10-7
英文名:GAMMA-SECRETASE INHIBITOR XII
中文名:Z-ILE-LEU-ALDEHYDE
CBNumber:CB0336194
分子式:C20H30N2O4
分子量:362.46
MOL File:161710-10-7.mol

Z-ILE-LEU-ALDEHYDE化学性质

沸点 :545.6±45.0 °C(Predicted)
密度 :1.074±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :insoluble in EtOH; insoluble in H2O; ≥10.8 mg/mL in DMSO
形态 :solid
酸度系数(pKa) :11.14±0.46(Predicted)
颜色 :White to off-white

Z-ILE-LEU-ALDEHYDE性质、用途与生产工艺

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

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.