| Name | WIKI4 |
| Description | WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2). |
| Kinase Assay | Recombinant human wild-type and mutant ALK kinase domain proteins (amino acids 1093–1411) are produced in-house using baculoviral expression, preactivated via autophosphorylation with MgATP, and assayed for kinase activity using a microfluidic mobility shift assay. The reactions contained 1.3 nM wild-type ALK or 0.5 nM mutant ALK (appropriate to produce 15-20% phosphorylation of peptide substrate after 1 h of reaction), 3 μM 5-FAM-KKSRGDYMTMQIG-CONH2), 5 mM MgCl2, and the Km level of ATP in 25 mM Hepes, pH 7.1. The inhibitors are shown to be ATP-competitive from kinetic and crystallographic studies. The Ki values are calculated by fitting the conversion (%) to a competitive inhibition equation. ROS1 enzyme is assayed as described above for ALK, except using 0.25 nM recombinant human ROS1 catalytic domain (amino acids 1883-2347). Kinase inhibitor selectivity is evaluated using a 206-kinase panel. |
| In vitro | WIKI4 inhibitsWnt/?-catenin signaling in all tested cell lines, including A375, DLD1 colorectal cancer, NALM6 B, U2OS osteosarcoma and hESCs. WIKI4 increases the steady-state abundance of theWnt/?-catenin inhibitory protein, AXIN1 by inhibiting tankyrase activity, and thus preventing the ubiquitylation and degradation of AXIN proteins.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 7.14 mg/mL (13.69 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | PARP | WIKI4 | poly ADP ribose polymerase | WIKI-4 | inhibit | Inhibitor | Beta catenin | β-catenin | WIKI 4 |
| Inhibitors Related | Urea | 4'-Methoxychalcone | Wnt pathway activator 1 | CHIR-99021 | 3-Aminobenzamide | XAV-939 | Niraparib | Olaparib | Benzamide | Nefopam hydrochloride | OUL35 | Bisdemethoxycurcumin |
| Related Compound Libraries | Bioactive Compound Library | Anti-Diabetic Compound Library | Anti-Obesity Compound Library | Anti-Breast Cancer Compound Library | Neuroprotective Compound Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
