TH1760

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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.

For research use only. We do not sell to patients.

TH1760 Chemical Structure

CAS No. : 2567914-01-4

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10 mg	USD 90	Ask For Quote & Lead Time
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Description

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.

2567914-01-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang SM, et al. Development of a chemical probe against NUDT15. Nat Chem Biol. 2020 Oct;16(10):1120-1128. [Content Brief]

[2]. Rehling D, et al. Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity. J Biol Chem. 2021 Jan-Jun;296:100568. [Content Brief]

TH1760 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TH17602567914-01-4TH 1760TH-1760Others6-TGHL-60 cellsHCT116 cellsAML HL-60 cellsInhibitorinhibitorinhibit

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