JW 55
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.
描述:IC50:1.9 μM(TNKS1);0.83 μM(TNKS2)。
β连环蛋白是经典Wnt信号的转导因子,β连环蛋白核积累的增加在许多肿瘤中出现,与肿瘤的发展和转移相关联。Wnt/β-catenin信号的抑制是抗癌药物有吸引力的战略。
体外实验:JW55是β-catenin信号通路的新型小分子抑制剂,通过抑制tankyrase 1和tankyrase 2(TNKS1/2)的PARP结构域而起作用。TNKS1/2是β-catenin破坏复合体的调节子。JW55对TNKS1/2聚ADP-核糖基化活性的抑制导致AXIN2的稳定化(β-catenin破坏复合体的成员),从而增加β-catenin的降解。在包含APC(腺瘤性结肠息肉病)位点突变或β-catenin等位基因突变的结肠癌细胞中,JW55以剂量依赖的方式抑制经典Wnt信号[1]。
体内实验:据报道,JW55减少爪蟾胚胎中XWnt8诱导的轴重复和APC突变小鼠中tamoxifen诱导的息肉形成。这些发现提供了一种新型的化合物,通过抑制TNKS1/2的PARP结构域,从而靶向经典Wnt/β-catenin信号通路[1]。
临床试验:JW55目前处于临床前开发阶段,没有进行中的临床试验。
参考文献:
[1] Waaler J, Machon O, Tumova L, Dinh H, Korinek V, Wilson SR, Paulsen JE, Pedersen NM, Eide TJ, Machonova O, Gradl D, Voronkov A, von Kries JP, Krauss S. A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice. Cancer Res. 2012;72(11):2822-32.
Physical Appearance | A solid |
Storage | Store at 4°C |
M.Wt | 434.48 |
Cas No. | 664993-53-7 |
Formula | C25H26N2O5 |
Solubility | insoluble in H2O; ≥19.25 mg/mL in DMSO; ≥3.53 mg/mL in EtOH with ultrasonic |
Chemical Name | N-[4-[[4-(4-methoxyphenyl)oxan-4-yl]methylcarbamoyl]phenyl]furan-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | COC1=CC=C(C=C1)C2(CCOCC2)CNC(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CO4 |
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。 |
JW 55是tankyrase 1和2(TNKS1/2)PARP结构域的抑制剂,减少TNKS1/2的自PARsylation,IC50值分别为1.9 μM和830 nM。 | ||||||
靶点 | TNKS1 | TNKS2 | ||||
IC50 | 1.9 uM | 830 nM |
质量控制和MSDS
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