TASIN-1 Hydrochloride 是一种截短型 APC 的选择性抑制剂，通过降低细胞胆固醇水平和通过结肠癌细胞中的 ER 应激/ROS/JNK 信号传导诱导凋亡细胞死亡来选择性杀死表达截短型 APC 的结肠直肠癌细胞。

TASIN-1 Hydrochloride is a selective inhibitor of truncated APC that acts by selectively killing colorectal cancer cells that express truncated APC by reducing cellular cholesterol levels and inducing apoptotic cell death through the ER stress/ROS/JNK signaling in colon cancer cells.

In nude mice with established DLD1 and HT29 tumors, intraperitoneal injection of TASIN-1 twice daily for 18 days reduced the size of tumor xenografts and tumor growth rates. TASIN-1 resulted in the appearance of apoptotic cells with fragmented nuclei and induced an increase in cleaved caspase 3 and cleaved PARP1. However, TASIN-1 did not inhibit tumor growth in HCT116 xenografts. In a genetically engineered CRC mouse model, TASIN-1 significantly reduced tumor formation in the colons of CPC [1].

1678515-13-3

C18H29ClN2O3S

388.95

TASIN 1 HCl;TASIN-1 HCl;塔辛-1盐酸盐;TASIN1 HCl

DMSO:55 mg/ml (141.41 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years