化合物TH1760 T67864

Product Introduction
Bioactivity


英文名: TH1760

描述: TH1760 (MKB) 是有效的 NUDIX-type 15 (NUDT15) 抑制剂 (IC50= 25 nM)。TH1760 可以通过增强核酸中 6-thio-(d) GTP 的积累增加细胞对 6-硫代鸟嘌呤的敏感程度。TH1760 增强了硫基嘌呤的抗白血病作用。

体外活性: TH1760 (0-100 µ M) maintained the thermal denaturation of NUDT15 in a dose-dependent manner. TH1760 (0, 5, 10, 20, and 50 µ M) increased the accumulation of thiopurine (6-TG) in a dose-dependent manner. TH1760 (10 µ M) increased the sensitivity of HCT116 and HCT116 3-6 cells to 6-TG. TH1760 has a higher sensitivity to BJ-RAS cells compared to BJ-hTERT cells. TH1760 (10 µ M; 16 h) promotes the accumulation and incorporation of 6-TG in HL-60 cells. TH1760 increased the expression of γ The expression of H2AX, caspase3, Cleared, and cPARP [1]. TH1760 (0.05, 0.17, 0.55, and 1.8 µ M; 4 d) enhanced the anti-leukemia effect of 6-TG in a dose-dependent manner [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 1.8 mg/mL (4.2 mM)


关键字: TH1760 | TH-1760 | TH 1760

相关产品: TH5427

相关库: Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途