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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Nucleoside Antimetabolite/Analog-TH7528
TH7528

Chemical Structure : TH7528

CAS No.:

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TH7528 (TH 7528)

货号: PC-21771Not For Human Use, Lab Use Only.

TH7528 (TH-7528) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 4.5, 2.8 and 2.6 uM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TH7528 (TH-7528) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 4.5, 2.8 and 2.6 uM, respectively.
TH7528 shows high selectivity against a panel of nucleotide phosphatases.
TH7528 impeded GTP-induced dimerization and thereafter activation, delayed the allosteric activation of SAMHD1.
TH7528 inhibited SAMHD1 hydrolase activity in vitro with low μM potencies and high selectivity, ia a mode of inhibition that deters efficient allosteric activation of SAMHD1 without occupying (d)NTP binding pockets.

物理化学性质&存储条件

分子量 321.40
分子式 C17H15N5S
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

N-(2-(pyridin-2-yl)ethyl)-6-(thiophen-2-yl)imidazo[1,2-a]pyrazin-8-amine

参考文献

1. Si Min Zhang, et al. iScience. 2024 Jan 13;27(2):108907.

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