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MW 521.6 Da, Purity >98%. WIKI-4 is a potent inhibitor of Wnt/β-catenin signaling EC50 ~ 75 nM (in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U-2 OS osteosarcoma cells, and hESCs); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM). Also a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively). It has little or no effect on related polymerases or transferases at 10 μM. Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway. WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.

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Key facts

CAS number
838818-26-1
Purity
> 98%
Form
Solid
Molecular weight
521.6 Da
Molecular formula
C29H23N5O3S
PubChem identifier
2984337
Nature
Synthetic

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MW 521.6 Da, Purity >98%. WIKI-4 is a potent inhibitor of Wnt/β-catenin signaling EC50 ~ 75 nM (in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U-2 OS osteosarcoma cells, and hESCs); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM). Also a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively). It has little or no effect on related polymerases or transferases at 10 μM. Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway. WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.

Key facts

Purity
> 98%
PubChem identifier
2984337
Solubility

Soluble in DMSO to 20 mM.

Biochemical name
2-[3-[[4-(4-Methoxyphenyl)-5-pyridin-4-yl-1,2,4-triazol-3-yl]sulfanyl]propyl]benzo[de]isoquinoline-1,3-dione
Biological description

WIKI-4 is a potent inhibitor of Wnt/β-catenin signaling EC50 ~ 75 nM (in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U-2 OS osteosarcoma cells, and hESCs); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM). Also a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively). It has little or no effect on related polymerases or transferases at 10 μM. Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway. WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells

Canonical SMILES
COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6
InChI
InChI=1S/C29H23N5O3S/c1-37-22-11-9-21(10-12-22)34-26(20-13-15-30-16-14-20)31-32-29(34)38-18-4-17-33-27(35)23-7-2-5-19-6-3-8-24(25(19)23)28(33)36/h2-3,5-16H,4,17-18H2,1H3
InChIKey
RNUXIZKXJOGYQP-UHFFFAOYSA-N
IUPAC name
2-[3-[[4-(4-methoxyphenyl)-5-pyridin-4-yl-1,2,4-triazol-3-yl]sulfanyl]propyl]benzo[de]isoquinoline-1,3-dione

Storage

Shipped at conditions
Blue Ice
Appropriate short-term storage duration
1-2 weeks
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark, Store under desiccating conditions

Notes

This product is manufactured by BioVision, an Abcam company and was previously called B1630 WIKI-4. B1630-25 is the same size as the 25 mg size of ab147053.

Protect from air and light.

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