MTH1
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S7505 | (S)-crizotinib | <1 mg/mL | 42 mg/mL | 22 mg/mL |
| S7631 | TH287 | <1 mg/mL | 53 mg/mL | 10 mg/mL |
| S7632 | TH588 | <1 mg/mL | 20 mg/mL | 1 mg/mL |
- MTH1 Inhibitors (3)
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7505 |
(S)-crizotinib(S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM in a cell-free assay. |
-crizotinib-S750501W0220161111.gif)
-crizotinib-S750501W0220161111.gif)
(B) Inhibition of ALK phosphorylation by alectinib in the Ba/F3 cell lines expressing mutated EML4-ALK. Cells were treated with alectinib or crizotinib for 2 h at the indicated concentrations. Phosphorylated ALK (Tyr 1604), ALK, and β-actin were detected by immunoblot analysis using antibodies to each of them.
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| S7631 |
TH287TH287 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 0.8 nM. |
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| S7632 |
TH588TH588 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 5 nM. It has no relevant inhibition of any of the other tested proteins at 100 μM, although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes, GPCRs, kinases, ion channels and transporters at 10 μM. |
Square wave voltammograms of C-DNA modified gold electrodes after incubation with different reaction solution that contains (a) active MTH1 (1.0 mg/mL), (b) inactivated MTH1 (1.0 mg/mL), (c) active MTH1 (1.0 mg/mL) with 10 μM TH588 inhibitor, and (d) hOGG1 (5.0 units).
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-crizotinib-Onco-Targets-Ther-20170112.gif)
