WIKI4

WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2[1][2]. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM[3].

Product Specifications

CAS Number

[838818-26-1]

UNSPSC

12352005

Hazard Statement

H302, H410

Target

PARP; Wnt; β-catenin

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/WIKI4.html

Purity

99.93

Solubility

DMSO : 6.8 mg/mL (ultrasonic; warming)

Smiles

O=C1N(CCCSC2=NN=C(C3=CC=NC=C3)N2C4=CC=C(OC)C=C4)C(C5=CC=CC6=CC=CC1=C56)=O

Molecular Formula

C29H23N5O3S

Molecular Weight

521.59

Precautions

H302, H410

References & Citations

[1]James RG, et al. WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling. PLoS One. 2012;7 (12) :e50457.|[2]Haikarainen T, et al. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4. PLoS One. 2013 Jun 6;8 (6) :e65404.|[3]Sadava D, et al. The effect of brassinolide, a plant steroid hormone, on drug resistant small-cell lung carcinoma cells. Biochem Biophys Res Commun. 2017 Nov 4;493 (1) :783-787.