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Autophinib
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。
Autophinib图片
CAS NO:1644443-47-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 346.73
Formula C14H11ClN6O3
CAS No. 1644443-47-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30mg/mL
Water: N/A
Ethanol: N/A
Chemical Name 6-Chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)pyrimidin-4-amine
Synonyms Autophinib
实验参考方法
In Vitro

In vitro activity: Autophinib is a novel and potent autophagy inhibitor, which inhibits starvation-induced or rapamyc induced autophagy. It acts by targeting the lipid kinase VPS34 with IC50 values of 90, 40 and 19 nM, respectively. Autophagy is a critical regulator of cellular homeostasis and metabolism. Interference with this process is considered a new approach for the treatment of disease, in particular cancer and neurological disorders. Therefore, novel small-molecule autophagy modulators such as autophinib are in high demand. Autophinib was identified by means of a phenotypic assay monitoring the formation of autophagy-induced puncta, indicating accumulation of the lipidated cytosolic protein LC3 on the autophagosomal membrane. Target identification and validation revealed that autophinib inhibits autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34.


Kinase Assay: Autophinib is a potent autophagy inhibitor, which can inhibit autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34 with IC50s of 90, 40 and 19 nM, respectively. Autophinib inhibits the accumulation of autophagosomes under fed as well as starved conditions, but does not affect the number of autolysosomes. Thus it is not a late stage autophagy inhibitor but an inhibitor of autophagosome formation. Autophinib targets VPS34 but not other lipid kinases, mTOR and TBK1. Autophinib appears to be ATP-competitive, targets VPS34 in cell lysate and induces cellular phenotypes consistent with VPS34 inhibition.


Cell Assay:

In Vivo
Animal model
Formulation & Dosage
References Angew Chem Int Ed Engl. 2017 Jul 3;56(28):8153-8157.