TH1760
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.
- CAS No.: 2567914-01-4
- Formula: C20H18N4O5S
- Molecular Weight:426.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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. Further protocols information, click here.
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Cell Line:HCT116 cells.
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Concentration:10 µM.
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Incubation Time:4 h.
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Result:Inhibited the expression of NUDT15.
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Cell Line:AML HL-60 cells.
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Concentration:10 µM.
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Incubation Time:3 h.
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Result:Significantly inhibited the expression of NUDT15 when the temperature was higher than 54℃.
Chemical Information
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CAS No. 2567914-01-4
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Molecular Weight 426.45
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Formula C20H18N4O5S
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SMILES
O=C1OC2=CC(S(=O)(N3CCN(CC3)C(C4=CC5=C(NC=C5)C=C4)=O)=O)=CC=C2N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TH1760 Related Classifications
HY-139193 Related Classifications
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