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Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM).

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $189 | 6-8 weeks | |
| 10 mg | $329 | 6-8 weeks | |
| 50 mg | $888 | 6-8 weeks | |
| 100 mg | $1,400 | 6-8 weeks |
| Description | Tankyrase Inhibitors 22 is a potent, selective, and orally bioavailable inhibitor of tankyrase (IC50: 0.1nM). |
| In vitro | Tankyrase inhibitors 22 is an optimization of the previous hit compound inhibitor 8 with improved potency and selectivity. It has excellent effects in both tankyrase assay and cellular assay (IC50: 0.1nM and 3.7nM, respectively). In addition, it is found to be a dual binder with both the nicotinamide pocket and the induced pocket of the enzymes [1]. |
| In vivo | In the in vivo studies in rodents, tankyrase inhibitors 22 is found to potently inhibit TNKS2 autoparsylation (IC50: 4.1nM). It also causes stabilization and accumulation of axin protein in SW480 cells (EC50: 3.9nM). In DLD-1 cells with truncated APC, the inhibitor inhibits the STF reporter transcription (IC50: 0.6nM) suggesting its downstream inhibitory activity on Wnt-associated transcription [1]. |
| Molecular Weight | 475.56 |
| Formula | C25H25N5O3S |
| Relative Density. | no data available |
| 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 mg/mL |

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