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Chemical Structure : TH1760
CAS No.: 2567914-01-4
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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|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $328 | In stock | |
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| 100 mg | Get quote |
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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.
| M.Wt | 426.447 | |
| Formula | C20H18N4O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
6-((4-(1H-indole-5-carbonyl)piperazin-1-yl)sulfonyl)benzo[d]oxazol-2(3H)-one |
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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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