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TH1760

Chemical Structure : TH1760

CAS No.: 2567914-01-4

TH1760 (TH 1760, TH-1760)

Catalog No.: PC-38226Not For Human Use, Lab Use Only.

TH1760 (TH 1760) is a first-in-class, potent, selective, cell-active NUDT15 inhibitor with IC50 of 25 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TH1760 (TH 1760) is a first-in-class, potent, selective, cell-active NUDT15 inhibitor with IC50 of 25 nM.
TH1760 displays no significant interaction and/or inhibition againstother human NUDIX proteins (MTH1, NUDT2, NUDT5, NUDT9, NUDT12, NUDT14, NUDT18 and NUDT22) and nucleotide pyrophosphatases (dCTPase, dUTPase and ITPase).
TH1760 sensitized cells to thiopurine in a NUDT15-dependent manner, through promoting intracellular accumulation and incorporation of 6-thio-dGTP.
At the tested concentration of 10 μM, TH1760 effectively engaged intracellular NUDT15 and further strongly potentiated its substrate thiopurines metabolites, without demonstrating apparent off-target toxicity.
TH1760 is a valuable tool to decipher the potential of NUDT15 inhibition in overcoming emerging resistance during thiopurine therapy.

Physicochemical Properties

M.Wt 426.447
Formula C20H18N4O5S
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-((4-(1H-indole-5-carbonyl)piperazin-1-yl)sulfonyl)benzo[d]oxazol-2(3H)-one

References

1. Zhang SM, et al. Nat Chem Biol. 2020 Oct;16(10):1120-1128.

2. Rehling D, et al. J Biol Chem. 2021 Jan-Jun;296:100568.

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