Name: USP7-IN-18
Brand: TargetMol
SKU: T211314
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

10-14周

50 mg

待询

10-14周

产品介绍

生物活性

产品描述	USP7-IN-18 (Compound X21) serves as a novel USP7 inhibitor by directly suppressing enzyme activity and modulating downstream pathways, including the newly identified PCLAF target. At concentrations of 0.25-1 μM for 24 hours, it exhibits inhibitory effects. USP7-IN-18 effectively reduces proliferation in leukemia (RS4;11) and colon cancer (MC38/CT26.WT) cells at 0.01-100 μM over 72 hours. It demonstrates high selectivity for USP7 at 2.5 μM within 0.5 hours, surpassing eight other deubiquitinating enzymes. SPR analysis shows that at 1.95-2000 nM for 3 minutes, the compound binds the catalytic domain of USP7 with a KD value of 4.9 μM.
体外活性	USP7-IN-18 (1.95-2000 nM, 3 min) 通过 SPR 分析显示与 USP7 的催化结构域结合，K D 值为 4.9 μM。USP7-IN-18 (Compound X21) (0.25-1 μM, 24 h) 是一种新型 USP7 抑制剂，通过直接抑制酶活性和调控下游通路（包括首次报道的 PCLAF 靶点）。在 USP7-IN-18 (0.01-100 μM, 72 h) 浓度下，显著抑制白血病 (RS4;11) 和结肠癌 (MC38/CT26.WT) 细胞的增殖。USP7-IN-18 (2.5 μM, 0.5 h) 具有对 USP7 的高度选择性，优于其他 8 种去泛素化酶。
体内活性	USP7-IN-18 (Compound X21) 以剂量5 mg/kg和10 mg/kg，每日一次、通过腹腔注射，持续16天，在携带MC38肿瘤的C57BL/6J小鼠模型中，能够显著抑制肿瘤生长。