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TH1760 (MKB) is an inhibitor of NUDIX-type 15 (NUDT15, IC50= 25 nM). TH1760 can sensitize cells to 6-thioguanine by increasing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 can enhance the anti-leukemia effect of thiopurine.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $50 | In Stock | In Stock | |
| 10 mg | $90 | In Stock | In Stock | |
| 25 mg | $210 | In Stock | In Stock | |
| 50 mg | $398 | In Stock | In Stock | |
| 100 mg | $592 | - | In Stock |
| Description | TH1760 (MKB) is an inhibitor of NUDIX-type 15 (NUDT15, IC50= 25 nM). TH1760 can sensitize cells to 6-thioguanine by increasing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 can enhance the anti-leukemia effect of thiopurine. |
| Targets&IC50 | NUDT15:25 nM |
| In vitro | TH1760 (0-100 µ M) maintained the thermal denaturation of NUDT15 in a dose-dependent manner. TH1760 (0, 5, 10, 20, and 50 µ M) increased the accumulation of thiopurine (6-TG) in a dose-dependent manner. TH1760 (10 µ M) increased the sensitivity of HCT116 and HCT116 3-6 cells to 6-TG. TH1760 has a higher sensitivity to BJ-RAS cells compared to BJ-hTERT cells. TH1760 (10 µ M; 16 h) promotes the accumulation and incorporation of 6-TG in HL-60 cells. TH1760 increased the expression of γ The expression of H2AX, caspase3, Cleared, and cPARP [1]. TH1760 (0.05, 0.17, 0.55, and 1.8 µ M; 4 d) enhanced the anti-leukemia effect of 6-TG in a dose-dependent manner [2]. |
| Synonyms | MKB |
| Molecular Weight | 426.45 |
| Formula | C20H18N4O5S |
| Cas No. | 2567914-01-4 |
| Smiles | S(=O)(=O)(C=1C=C2C(=CC1)NC(=O)O2)N3CCN(C(=O)C=4C=C5C(=CC4)NC=C5)CC3 |
| Relative Density. | 1.534 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: 1.8 mg/mL (4.22 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
| |||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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