OTSSP167 hydrochloride
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.
OTSSP167是一种母系胚胎亮氨酸拉链蛋白激酶(MELK)抑制剂,其IC50值为0.41 nM[1].
MELK属于AMPK丝氨酸/苏氨酸激酶家族,参与哺乳动物胚胎发育.MELK在多种人类癌症中过表达.OTSSP167是通过高通量筛选得到的.体外抗增殖试验表明,OTSSP167抑制多种癌细胞系生长,如A549(IC50 = 6.7 nM)\T47D(IC50 = 4.3 nM)\DU4475(IC50 = 2.3 nM)以及22Rv1(IC50 = 6.0 nM).体内试验显示,在各种癌细胞系异种移植模型中,OTSSP167可以显著抑制肿瘤生长.静脉注射与口服给药后,均观察到上述作用.当使用MELK的底物时,OTSSP167在体外抑制DBNL与PSMA1的磷酸化.由于PSMA1对癌细胞生存是必需的,因而OTSSP167引起的磷酸化PSMA1的减少可以抑制肿瘤干细胞微球体形成[1].
参考文献：
[1] Suyoun Chung, Hanae Suzuki, Takashi Miyamoto et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012, 3: 1629-1640.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 523.88 |
| Cas No. | 1431698-10-0 |
| Formula | C25H29Cl3N4O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | 4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichlorocyclohexa-2,5-dien-1-one;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC(=O)C1=CN=C2C=CC(=C3C=C(C(=O)C(=C3)Cl)Cl)NC2=C1NC4CCC(CC4)CN(C)C.Cl |
| 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。 |
| Description | OTSSP167 hydrochloride是有效的母系胚胎亮氨酸拉链蛋白激酶(MELK)抑制剂,其IC50值为0.41 nM. | |||||
| 靶点 | MELK | |||||
| IC50 | 0.41nM | |||||
化学结构
