For research use only. Not for therapeutic Use.
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].
WIKI4 (100 nM, 1 μM; 6 days; DLD1 cells) inhibits growth of DLD1 cells relative to DMSO controls in media containing low serum. WIKI4 inhibits expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling[1].
WIKI4 (1 μM; 2 hours, 4 hours, 6 hours, or 24 hours; DLD1 cells) significantly increases the steady-state abundance of AXIN1 and AXIN2[1].
| Catalog Number | I005023 |
| CAS Number | 838818-26-1 |
| Synonyms | 2-[3-[[4-(4-methoxyphenyl)-5-pyridin-4-yl-1,2,4-triazol-3-yl]sulfanyl]propyl]benzo[de]isoquinoline-1,3-dione |
| Molecular Formula | C29H23N5O3S |
| Purity | ≥95% |
| 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 |
| SMILES | COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6 |
| Reference | [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. |
