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Vacquinol-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vacquinol-1图片
CAS NO:5428-80-8
包装:5mg
市场价:1061元

产品介绍
Vacquinol-1 (NSC13316) 是一种 MKK4 特异性激活剂,可激活 MAPK 通路。 Vacquinol-1 在多形性胶质母细胞瘤 (GBM) 小鼠模型中特异性诱导人胶质母细胞瘤细胞 (GC) 死亡、减缓肿瘤进展并延长生存期。 Vacquinol-1 还诱导肝细胞癌 (HCC) 细胞凋亡。
Cas No.5428-80-8
别名NSC13316
化学名(2-(4-chlorophenyl)quinolin-4-yl)(piperidin-2-yl)methanol
Canonical SMILESOC(C1=CC(C2=CC=C(Cl)C=C2)=NC3=CC=CC=C13)C4NCCCC4
分子式C21H23Cl3N2O
分子量425.78
溶解度DMF: 10 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 1 mg/ml,Ethanol: 0.25 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 3.14 μM for glioma cells

Vacquinol-1 is a MAPK kinase 4 (MKK4) activator.

Mitogen-activated protein kinase (MAPK) is a type of protein kinase that is specific to the amino acids serine, threonine, and tyrosine. MAPKs regulate cell functions such asgene expression, mitosis, proliferation, differentiation, cell survival, as well as apoptosis.

In vitro: Previous study showed that vacquinol-1 displayed high cytotoxicity against glioma cells, resulting in a complete loss of viability as measured by ATP depletion. Vacquinol-1 could selectively target GCs in mixed cocultures with human fibroblasts. Moreover, vacquinol-1 had no effect on caspase activity at any concentration or time point, which was unlike that of staurosporin. In addition, the fluorescence staining and western blot analyses of GCs for activating MKK4 phosphorylation revealed a rapid and pronounced activation by vacquinol-1 at 7.5 μM [1].

In vivo: The ability of vacquinol-1 to attenuate tumor progression was previously tested in a mouse model for human GBM. Vacquinol-1 or vehicle (DMSO) were intracranially administered into the site of original cell deposit 6 weeks after engraftment. Results showed that tumors were invariantly smaller, and the area of necrosis and hGFAP and hNestin immunoreactivity was significantly reduced. Moreove, only tumor cells in vacquinol-1-treated mice showed a massive LAMP1 staining [1].

Clinical trial: Up to now, vacquinol-1 is still in the preclinical development stage.

Reference:
[1] Kitambi SS et al.  Vulnerability of glioblastoma cells to catastrophic vacuolization and death induced by a small molecule. Cell. 2014 Apr 10;157(2):313-28.