Chemical Structure : Cathepsin D inhibitor N-8
CAS No.:
Cathepsin D inhibitor N-8
货号: PC-25342Not For Human Use, Lab Use Only.
Cathepsin D inhibitor N-8 is a potent, specific inhibitor of Cathepsin D (CTSD) with SPR KD of 0.58 uM, effectively inhibits proliferation and induces apoptosis in leukemia cells with high CTSD expression.
大包装，大折扣！
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
Cathepsin D inhibitor N-8 is a potent, specific inhibitor of Cathepsin D (CTSD) with 1SPR KD of 0.58 uM, effectively inhibits proliferation and induces apoptosis in leukemia cells with high CTSD expression.
N-8 demonstrates potent inhibitory activity in U937 cells with IC50 of 5.895 uM.
N-8 effectively inhibits proliferation of MV4-11 and MOLM-13 cells with IC50 values (IC5==5.9-11.4 uM) in the micromolar range and exerted similar effects in venetoclax-resistant AML cells (MOLM-13-VEN-R and MV4-11-VEN-R).
N-8 induces apoptosis in both AML cells and venetoclax-resistant AML cells in a dose-dependent manner, also showed significant pro-apoptotic activity in primary AML cells.
N-8 inhibits AML by promoting TRIM21-mediated degradation of the anti-apoptotic proteins BCL2, BCL-XL, and MCL1.
N-8 (30 mg/kg, PO, QD) attenuates the progression of AML in mice xenografted with U937 AML cells (AML mice), reduces BCL2, BCL-XL, and MCL1 expression in spleen and BM cells.
物理化学性质&存储条件
|
分子量
|
362.56
|
|
分子式
|
C25H34N2
|
|
外观性状
|
Solid
|
|
CAS No.
|
|
|
储存条件
|
- 固体粉末
-
-20°C 12 个月; 4°C 6 个月
|
- 配置液
-
-80°C 6 个月; -20°C 6 个月
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
2-(4-(tert-butyl)phenyl)-5-(2,4,4-trimethylpentan-2-yl)-1H-benzo[d]imidazole
|
参考文献
1. Jiang H, et al. Cell Death Dis. 2025 Aug 12;16(1):611.
