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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA Repair Protein -TH1760
TH1760

Chemical Structure : TH1760

CAS No.: 2567914-01-4

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TH1760 (TH 1760, TH-1760)

货号: PC-38226Not For Human Use, Lab Use Only.

TH1760 (TH 1760) is a first-in-class, potent, selective, cell-active NUDT15 inhibitor with IC50 of 25 nM.

规格 价格 库存 数量
10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TH1760 (TH 1760) is a first-in-class, potent, selective, cell-active NUDT15 inhibitor with IC50 of 25 nM.
TH1760 displays no significant interaction and/or inhibition againstother human NUDIX proteins (MTH1, NUDT2, NUDT5, NUDT9, NUDT12, NUDT14, NUDT18 and NUDT22) and nucleotide pyrophosphatases (dCTPase, dUTPase and ITPase).
TH1760 sensitized cells to thiopurine in a NUDT15-dependent manner, through promoting intracellular accumulation and incorporation of 6-thio-dGTP.
At the tested concentration of 10 μM, TH1760 effectively engaged intracellular NUDT15 and further strongly potentiated its substrate thiopurines metabolites, without demonstrating apparent off-target toxicity.
TH1760 is a valuable tool to decipher the potential of NUDT15 inhibition in overcoming emerging resistance during thiopurine therapy.

物理化学性质&存储条件

分子量 426.447
分子式 C20H18N4O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-((4-(1H-indole-5-carbonyl)piperazin-1-yl)sulfonyl)benzo[d]oxazol-2(3H)-one

参考文献

1. Zhang SM, et al. Nat Chem Biol. 2020 Oct;16(10):1120-1128.

2. Rehling D, et al. J Biol Chem. 2021 Jan-Jun;296:100568.

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