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.
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- CAS. Nr.: 2567914-01-4
- Formel: C20H18N4O5S
- Molecular Weight:426.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
NUDIX-type 15, NUDT15[1]
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.
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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. Nr. 2567914-01-4
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Molecular Weight 426.45
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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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)
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
TH1760 Related Classifications
HY-139193 Related Classifications
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