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TH6342

Chemical Structure : TH6342

CAS No.:

TH6342 (TH 6342, TH-6342, CBK037371)

Catalog No.: PC-21770Not For Human Use, Lab Use Only.

TH6342 (TH-6342) 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 9.6, 11.0 and 5.8 uM, respectively.

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Biological Activity

TH6342 (TH-6342) 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 9.6, 11.0 and 5.8 uM, respectively.
TH6342 shows high selectivity against a panel of nucleotide phosphatases.
TH6342 impeded GTP-induced dimerization and thereafter activation, delayed the allosteric activation of SAMHD1.
TH6342 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

M.Wt 349.82
Formula C19H16ClN5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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