2567914-01-4
2567914-01-4 structure
- Name: TH1760
- Chemical Name: TH1760
- CAS Number: 2567914-01-4
- Molecular Formula: C20H18N4O5S
- Molecular Weight: 426.45
- Catalog: Research Areas Cancer
- Create Date: 2023-05-23 11:52:30
- Modify Date: 2024-11-30 12:05:55
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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].
| Name | TH1760 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
NUDIX-type 15, NUDT15[1] |
| 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]。 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℃. |
| References |
| Molecular Formula | C20H18N4O5S |
|---|---|
| Molecular Weight | 426.45 |