| Name | NVP-TNKS656 |
| Description | NVP-TNKS656 (TNKS656) is a highly potent, selective, and orally active TNKS2 inhibitor. |
| In vitro | In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. [1] In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis. [2] |
| In vivo | In mice, NVP-TNKS656 displays low clearance and volume of distribution, and exhibits good exposure and moderate oral bioavailability. In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 (350 mg/kg, p.o.) stabilizes Axin1 protein and reduces the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. [1] In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. [2] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 93 mg/mL (188.04 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.67 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 10 mg/mL (20.22 mM), Heating is recommended.
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| Keywords | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | TNKS-656 | TNKS2 | TNKS 656 | poly ADP ribose polymerase | PARP | NVP-TNKS-656 | NVP-TNKS656 | NVPTNKS656 | NVP-TNKS 656 | NVP TNKS656 | Inhibitor | inhibit | beta-catenin | betacatenin | bcatenin | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Ethyl linoleate | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Colorectal Cancer Compound Library | Osteogenesis Compound Library | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Prostate Cancer Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
