OTS514
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.
OTS514,噻吩并[2,3-c]喹诺酮类化合物,是一种高效的TOPK抑制剂,IC50值为2.6 nM。OTS514可以抑制TOPK激酶活性。TOPK(T - 淋巴因子激活的杀伤细胞来源的蛋白激酶)是一种蛋白质,在多种人类癌症中被发现,被认为是一个原癌基因,促进肿瘤的生长。
据报道,OTS514强烈抑制TOPK阳性癌细胞系的生长,IC50范围介于1.5-14 nM之间。在几乎检测不到TOPK表达的HT29细胞中,IC50值为170 nM。OTS514以1、2.5和5 mg/kg的剂量每天一次静脉给药,持续给药2周后分别导致了5.7%、43.3%和65.3%的肿瘤生长抑制(TGI),没有任何体重的损失。然而,这种抑制也会引起造血干细胞(HSCs)向白细胞和红细胞分化的功能障碍,但可能会增强造血干细胞向巨核细胞和血小板的分化。
在LU-99癌细胞异种移植小鼠中,当肿瘤体积达到200 mm3时,OTS514 (5 mg/kg)以静脉注射的方式每天一次持续给药2周展示了很好的肿瘤生长抑制效应(TGI,104%),没有任何体重的损失。而且,OTS514的抗肿瘤效应还会引起白细胞数量的显著减少。
参考文献:
1. Matsuo Y, Park JH2, Miyamoto T, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. ci Transl Med. 2014 Oct 22;6(259):259ra145.
2. Y. Nakamura, Y. Matsuo, S. Hisada, et al. Tricyclic compounds and PBK inhibitors containing the same. Patent WO/2011/123419 (2011)
Storage | Store at -20°C |
M.Wt | 350.43 |
Cas No. | 1338540-55-8 |
Formula | C20H18N2O2S |
Solubility | Soluble in DMSO |
Chemical Name | (R)-9-(4-(1-aminopropan-2-yl)phenyl)-8-hydroxythieno[2,3-c]quinolin-4(5H)-one |
SDF | Download SDF |
Canonical SMILES | NC[C@H](C)C1=CC=C(C2=C(O)C=CC3=C2C(C=CS4)=C4C(N3)=O)C=C1 |
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。 |