161710-10-7
中文名稱
Z-ILE-LEU-ALDEHYDE
英文名稱
GAMMA-SECRETASE INHIBITOR XII
CAS
161710-10-7
分子式
C20H30N2O4
分子量
362.46
MOL 文件
161710-10-7.mol
161710-10-7 結(jié)構(gòu)式
基本信息
中文別名
GAMMA-SECRETASE抑制劑(Z-ILE-LEU-ALDEHYDE) 英文別名
GSI-XII)Z-IL-CHO
Z-ILE-LEU-ALDEHYDE
Z-Ile-Leu-aldehyde(Z-IL-CHO
GAMMA-SECRETASE INHIBITOR XII
γ-Secretase inhibitor XII (GSI-XII)
Z-ILE-LEU-ALDEHYDE(Z-IL-CHO
GSI-XII)
Z-IL-CHO
GSI-XII
Γ-SECRETASE INHIBITOR XII
Benzyl ((2S,3S)-3-methyl-1-(((S)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)carbamate
Carbamic acid, N-[(1S,2S)-1-[[[(1S)-1-formyl-3-methylbutyl]amino]carbonyl]-2-methylbutyl]-, phenylmethyl ester
物理化學(xué)性質(zhì)
沸點(diǎn)545.6±45.0 °C(Predicted)
密度1.074±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度insoluble in EtOH; insoluble in H2O; ≥10.8 mg/mL in DMSO
酸度系數(shù)(pKa)11.14±0.46(Predicted)
形態(tài)固體
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
Z-Ile-Leu-aldehyde (Z-IL-CHO) 是有效的、競(jìng)爭(zhēng)性的 γ-secretase 和 notch 的肽醛抑制劑。體外研究
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 |
體內(nèi)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. |