货号:A631906
同义名:
GSII; Z-Leu-Leu-Nle-CHO
Z-LLNle-CHO是一种 γ-Secretase 抑制剂,通过阻断 Akt 促生存通路并诱导 ROS 和 caspase 依赖的细胞凋亡,广泛应用于癌症研究,特别是乳腺癌和白血病研究。
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产品名称 | 20S proteasome ↓ ↑ | Proteasome ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ixazomib |
++++
20S proteasome, Ki: 0.93 nM 20S proteasome, IC50: 3.4 nM |
99%+ | |||||||||||||||||
Delanzomib |
+++
Chymotrypsin-like proteasome, IC50: 3.8 nM |
98% | |||||||||||||||||
Celastrol |
+
20S proteasome, IC50: 2.5 μM |
98% | |||||||||||||||||
MLN9708 |
+++
20S proteasome, Ki: 0.93 nM 20S proteasome, IC50: 3.4 nM |
99% | |||||||||||||||||
Bortezomib |
++++
20S proteasome, Ki: 0.6 nM |
98% | |||||||||||||||||
Oprozomib |
++
20S proteasome β5, IC50: 36 nM 20S proteasome LMP7, IC50: 82 nM |
99%+ | |||||||||||||||||
Epoxomicin | ✔ | 95% | |||||||||||||||||
PI-1840 |
++
Chymotrypsin-like proteasome, IC50: 27 nM |
98% | |||||||||||||||||
VR23 |
+++
Trypsin-like proteasomes, IC50: 1 nM Chymotrypsin-like proteasomes, IC50: 3 μM |
99% | |||||||||||||||||
Carfilzomib |
++
Proteasome, IC50: 5 nM |
98% | |||||||||||||||||
(R)-MG-132 |
+
Proteasome, IC50: 100 nM |
98% (NMR) | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Z-LLNle-CHO is a γ-secretase inhibitor. Z-LLNle-CHO induces caspase- and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway and can be used in cancer research such as breast cancer and leukaemia[1][2].Z-LLNle-CHO caused inhibition of cell viability/proliferation in a dose-dependent manner in six breast cancer cell lines tested at concentrations of 0-5 µM. Z-LLNle-CHO has proteasome inhibitory activity and is cytotoxic to MCF-7 cells[1].Z-LLNle-CHO blocks the Akt-mediated pro-survival pathway and induces Caspase- and ROS-dependent apoptosis in Nalm6 and 697 cells[2]. |
Animal study | At a dose of 5 mg/kg administered subcutaneously once daily for 12 days, Z-LLNle-CHO inhibits engraftment of B lymphocytes in the precursor-B ALL xenograft model[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.10mL 0.42mL 0.21mL |
10.51mL 2.10mL 1.05mL |
21.03mL 4.21mL 2.10mL |
CAS号 | 133407-83-7 |
分子式 | C26H41N3O5 |
分子量 | 475.62 |
SMILES Code | O=C(N[C@@H](CC(C)C)C(N[C@@H](CCCC)C=O)=O)[C@H](CC(C)C)NC(OCC1=CC=CC=C1)=O |
MDL No. | MFCD02179375 |
别名 | GSII; Z-Leu-Leu-Nle-CHO; gamma-Secretase Inhibitor I. Z-Leu-Leu-Nle-CHO (Nle = Norleucine). |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, store in freezer, under -20°C |