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TH1760 是一种 NUDIX-type 15 (NUDT15) 抑制剂,IC50 值为 25 nM。TH1760 通过增强核酸中 6-thio-(d) GTP 的积累使细胞对 6-硫代鸟嘌呤敏感。TH1760 增强了硫基嘌呤的抗白血病作用。

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TH1760 Chemical Structure

TH1760 Chemical Structure

CAS No. : 2567914-01-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine[1][2].

IC50 & Target

NUDIX-type 15, NUDT15[1]

体外研究
(In Vitro)

TH1760 (0-100 µM) 以剂量依赖的方式维持了 NUDT15 的热变性[1]
TH1760 (0、5、10、20 和 50 µM) 以剂量依赖的方式增加了硫基嘌呤 (6-TG) 的积累[1]
TH1760 (10 µM) 增加了 HCT116 和 HCT116 3-6 细胞对 6-TG 的敏感性。TH1760 对 BJ-RAS 细胞致敏性更高相比于 BJ-hTERT 细胞[1]
TH1760 (10 µM;16 h) 促进 6-TG 在 HL-60 细胞中的积累与掺入。TH1760 增加了 HL-60 细胞中 γH2AX、caspase3、Cleaved 和 cPARP 的表达[1]
TH1760 (0.05、0.17、0.55 和 1.8 µM;4 d) 以剂量依赖的方式增强了 6-TG 的抗白血病作用[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCT116 cells.
Concentration: 10 µM.
Incubation Time: 4 h.
Result: Inhibited the expression of NUDT15.

Western Blot Analysis[2]

Cell Line: AML HL-60 cells.
Concentration: 10 µM.
Incubation Time: 3 h.
Result: Significantly inhibited the expression of NUDT15 when the temperature was higher than 54℃.
分子量

426.45

Formula

C20H18N4O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

TH1760 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-139193
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