Chemical Structure : TH7528
CAS No.:
TH7528
(TH 7528)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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321.40
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Formula
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C17H15N5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(2-(pyridin-2-yl)ethyl)-6-(thiophen-2-yl)imidazo[1,2-a]pyrazin-8-amine
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References
1. Si Min Zhang, et al. iScience. 2024 Jan 13;27(2):108907.
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