TH1760|CAS 2567914-01-4|DC Chemicals

Cas No.:	2567914-01-4
Chemical Name:	2(3H)-Benzoxazolone, 6-[[4-(1H-indol-5-ylcarbonyl)-1-piperazinyl]sulfonyl]-
SMILES:	C1C2NC=CC=2C=C(C(N2CCN(S(=O)(=O)C3C=CC4NC(=O)OC=4C=3)CC2)=O)C=1
Formula:	C₂₀H₁₈N₄O₅S
M.Wt:	426.45
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	TH1760 is a first-in-class, potent, selective and cell-active NUDT15 (MTH2) inhibitor with an IC50 value of 25 nM.
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:	[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.

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