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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 | Backorder | |
10 mg | $329 | Backorder | |
50 mg | $888 | Backorder | |
100 mg | $1,400 | Backorder |
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. |
Solubility Information | DMSO: <1 mg/mL |
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