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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $189 | 6-8 weeks | 6-8 weeks | |
| 10 mg | $329 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $888 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $1,400 | 6-8 weeks | 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 |
| Smiles | O=C1NC(SCCC(N[C@H]2CC[C@H](C3=NN=C(C4=CC=CC=C4)O3)CC2)=O)=NC5=CC=CC=C51 |
| 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 |
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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