TH1217(Synonyms: ZINC1775962367)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TH1217 (Synonyms: ZINC1775962367)

TH1217 (ZINC1775962367) 是一种有效的、选择性的 dCTPase pyrophosphatase 1 (dCTPase) 抑制剂，IC50 值为 47 nM。TH1217 可增强胞苷类似物在白血病细胞中的细胞毒性作用。TH1217 还可以调节 SARS-Cov-2 相互作用体，因此它具有抗 COVID-19 的活性。

TH1217(Synonyms: ZINC1775962367)

TH1217 Chemical Structure

CAS No. : 1862212-48-3

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生物活性

TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[1][2].

IC50 & Target

IC50: 47 nM (dCTPase)[1]
体外研究
(In Vitro)

TH1217 (compound 30) inhibits dCTPase and enhances aqueous solubility (>100 μM) and improves plasma stability in vitro(t4h=86%)[1].
TH1217 presents suitable mouse microsomal half-lives (109 minutes)[1].
TH1217 displays well cell permeability (8.66×10-6/1.30×10-3 cm/s) and CYP inhibition[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

491.09

Formula

C20H17BCl2N4O6
CAS 号

1862212-48-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Llona-Minguez S, et, al. Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1. Med Chem. 2016 Feb 11; 59(3): 1140-1148.

    [2]. Gordon DE, et, al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22; 2020.03.22.002386.

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