ZLDI-8 是 Notch 激活/裂解酶 ADAM-17 的抑制剂,可抑制 Notch 蛋白裂解,并降低促存活/抗凋亡和上皮-间质转化相关蛋白的表达。它还是竞争性不可逆酪氨酸磷酸酶抑制剂,以IC50为 5.32 μM 抑制 MHCC97-H 细胞的生长。
产品描述
ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.
体外活性
ZLDI-8;?it inhibited the cleavage of NOTCH protein, consequently decreased the expression of pro-survival/anti-apoptosis and EMT related proteins.?ZLDI-8 treatment enhanced the susceptibility of HCC cells to a small molecular kinase inhibitor Sorafenib, and chemotherapy agents Etoposide and Paclitaxel.?ZLDI-8 treatment enhanced the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model[1].
体内活性
In nude HCC-bearing mice model, ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth [1].
Cas No.
667880-38-8
分子式
C24H23N3O3S
分子量
433.52
储存和溶解度
DMSO:62.5 mg/mL (144.17 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years