TH5427 在NUDT5 活性和 ADP-核糖代谢中有研究的价值。它阻断孕激素依赖性、PAR 衍生的核 ATP 合成以及随后的乳腺癌细胞染色质重塑、基因调控和增殖。NUDT5是乳腺癌细胞激素依赖性基因调控和增殖的变阻器。

TH5427 is a lead NUDT5 inhibitor(MG assay IC50 = 29 nM).

In HL-60 cell lysates, TH5427(20?μM) stabilized NUDT5 to nearly the same levels as observed in the 37?°C DMSO control. TH5427 was the most potent stabilizer under the described conditions with an apparent EC50 of 2.1?μM. Accordingly, TH5427 had a positive, dose-dependent shift in the apparent Tagg—the temperature at which 50 % of the target protein denatures and aggregates (TH5427 shifted NUDT5 Tagg up to?≈?8?°C)[1].

2253744-56-6

(< 1 mg/ml refers to the product slightly soluble or insoluble )
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