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Key Documents

SML0760

Sigma-Aldrich

WIKI4

≥98% (HPLC)

Synonym(s):

2-[3-[[4-(4-Methoxyphenyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]propyl]-1Hbenz[de]isoquinoline-1,3(2H)-dione

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About This Item

Empirical Formula (Hill Notation):
C29H23N5O3S
CAS Number:
838818-26-1
Molecular Weight:
521.59
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear (warmed)

storage temp.

−20°C

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

InChI key

RNUXIZKXJOGYQP-UHFFFAOYSA-N

Biochem/physiol Actions

WIKI4 is a potent inhibitor of Wnt/β-catenin signaling with an EC50 ~ 75 nM in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U2OS osteosarcoma cells, and hESCs. WIKI4 inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) with an IC50 of 15 nM, preventing the ubiquitination and degradation of axin and thereby antagonizing Wnt signalling.

Features and Benefits

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Certificates of Analysis (COA)

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Sukyeong Kim et al.
Nature communications, 10(1), 4898-4898 (2019-10-28)
Osteoarthritis (OA) is a prevalent degenerative disease, which involves progressive and irreversible destruction of cartilage matrix. Despite efforts to reconstruct cartilage matrix in osteoarthritic joints, it has been a difficult task as adult cartilage exhibits marginal repair capacity. Here we

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