| Bioactivity | 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]. |
| Target | NUDIX-type 15, NUDT15 |
| Invitro | 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: |
| Name | TH1760 |
| CAS | 2567914-01-4 |
| Formula | C20H18N4O5S |
| Molar Mass | 426.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhang SM, et al. Development of a chemical probe against NUDT15. Nat Chem Biol. 2020 Oct;16(10):1120-1128. [2]. Rehling D, et al. Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity. J Biol Chem. 2021 Jan-Jun;296:100568. |