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TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine.

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TH1760 Chemical Structure

TH1760 Chemical Structure

CAS No. : 2567914-01-4

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Description

TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine[1][2].

IC50 & Target

NUDIX-type 15, NUDT15[1]

In Vitro

TH1760 (0-100 µM) maintains the thermal denaturation of NUDT15 with dose-dependent manner[1].
TH1760 (0, 5, 10, 20 and 50 µM) increases the accumulation of thiopurine (6-TG) with dose-dependent manner in NB4 and HL-60 cells[1].
TH1760 (10 µM) increases the sensitivity of HCT116 and HCT116 3-6 cells to 6-TG. TH1760. TH1760 is more sensitive to BJ-RAS cells than BJ-hTERT cells[1].
TH1760 (10 µM; 16 h) promotes the accumulation and incorporation of 6-TG in HL-60 cells. TH1760 increases the expression of γH2AX, caspase3, Cleaved and cPARP in HL-60 cells[1].
TH1760 (0.05, 0.17, 0.55 and 1.8 µM; 4 d) enhances the anti-leukemia effect of 6-TG in a dose dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCT116 cells.
Concentration: 10 µM.
Incubation Time: 4 h.
Result: Inhibited the expression of NUDT15.

Western Blot Analysis[2]

Cell Line: AML HL-60 cells.
Concentration: 10 µM.
Incubation Time: 3 h.
Result: Significantly inhibited the expression of NUDT15 when the temperature was higher than 54℃.
Molecular Weight

426.45

Formula

C20H18N4O5S

CAS No.
SMILES

O=C1OC2=CC(S(=O)(N3CCN(CC3)C(C4=CC5=C(NC=C5)C=C4)=O)=O)=CC=C2N1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TH1760 Related Classifications

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Product Name:
TH1760
Cat. No.:
HY-139193
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