JW 74
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 790 nM for canonical Wnt signaling
JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2.
Wnt/β-catenin, a major regulator of stem cell self-renewal and differentiation, is aberrantly activated in a several cancers, including osteosarcoma. Thus, attenuation of Wnt/β-catenin activity by tankyrase inhibitors is an appealing strategy in osteosarcoma treatment.
In vitro: Previous study found that JW74 at the molecular level induced stabilization of AXIN2, a key component of the β-catenin destruction complex, leading to reduced levels of nuclear β-catenin. In addition, JW74 could induce reduced cell growth in all tested cell lines, partially due to a delay in cell cycle progression and partially because of an induction of caspase-3-mediated apoptosis. Moreover, JW74 was able to induce the differentiation in U2OS cells and also enhance differentiation of OS cell lines that did not harbor a differentiation block [1].
In vivo: Previous animal study found that the dose of 150 mg/kg of JW74 in ApcMin model could reduce the small intestinal adenoma by 48% and was comparable with celecoxib or rofecoxib. Furthermore, it was noteworthy that JW74 became rapidly cleared from the blood stream due to its poor in vivo stability [2].
Clinical trial: Up to now, JW 74 is still in the preclinical development stage.
References:
1. E. W. Stratford, J. Daffinrud, E. Munthe, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 3(1), 36-46 (2014).
2. Waaler J et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 456.5 |
Cas No. | 863405-60-1 |
Formula | C24H20N6O2S |
Solubility | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | 4-[4-(4-methoxyphenyl)-5-[[[3-(4-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]thio]-4H-1,2,4-triazol-3-yl]-pyridine |
SDF | Download SDF |
Canonical SMILES | CC(C=C1)=CC=C1C2=NOC(CSC3=NN=C(C4=CC=NC=C4)N3C5=CC=C(OC)C=C5)=N2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |