Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 57.00 | |
10 mg | In stock | $ 84.00 | |
25 mg | In stock | $ 161.00 | |
50 mg | In stock | $ 298.00 | |
100 mg | In stock | $ 493.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 72.00 |
Description | WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2). |
Targets&IC50 | TNKS2:15 nM |
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] |
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. |
Molecular Weight | 521.59 |
Formula | C29H23N5O3S |
CAS No. | 838818-26-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.14 mg/mL (13.69 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
WIKI4 838818-26-1 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin poly ADP ribose polymerase WIKI-4 inhibit Inhibitor Beta catenin β-catenin WIKI 4 inhibitor