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WIKI4

WIKI4
WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2).
Catalog No. T3062Cas No. 838818-26-1
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Purity:99.6%
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WIKI4

Catalog No. T3062Cas No. 838818-26-1
WIKI4 is a potent inhibitor of Wnt/β-catenin signaling and tankyrase 2 (TNKS2).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$34In Stock
10 mg$48In Stock
25 mg$97In Stock
50 mg$179In Stock
100 mg$296In Stock
200 mg$429In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight521.59
FormulaC29H23N5O3S
Cas No.838818-26-1
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9172 mL9.5861 mL19.1721 mL95.8607 mL
5 mM0.3834 mL1.9172 mL3.8344 mL19.1721 mL
10 mM0.1917 mL0.9586 mL1.9172 mL9.5861 mL

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