product name WIKI4
Description: WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling. WIKI4 inhibits expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in cancer cell lines as well as in human embryonic stem cells. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2, a regulator of AXIN ubiquitylation and degradation. While TNKS has previously been shown to be the target of small molecule inhibitors of Wnt/β-catenin signaling, WIKI4 is structurally distinct from previously identified TNKS inhibitors.
References: PLoS One. 2012;7(12):e50457.
521.59
Formula
C29H23N5O3S
CAS No.
838818-26-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 7 mg/mL (13.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: WIKI4 inhibitsWnt/ß-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/ß-catenin inhibitory protein, AXIN1 by inhibiting tankyrase activity, and thus preventing the ubiquitylation and degradation of AXIN proteins. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | PLoS One. 2012;7(12):e50457. |
