3-Methyladenine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种针对 Vps34 和 PI3Kγ 的选择性 PI3K 抑制剂，在 HeLa 细胞中的 IC50 分别为 25 uM 和 60 uM。

A selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 uM and 60 uM in HeLa cells; blocks class I PI3K persistently, whereas its suppressive effect on class III PI3K is transient; induces caspase-dependent cell death in HeLa cells, and the death occurs independently of the inhibition of autophagy; also blocks autophagosome formation.(In Vitro):3-Methyladenine (0-10 mM; 0-48 hours) induces caspase-dependent cell death in HeLa cells in a time-and dose-dependent manner.3-Methyladenine (5 mM; 24 hours) suppresses autophagy in HeLa cells under both glucose-free conditions and normal conditions.3-Methyladenine (5 mM; 0-48 hours) suppresses conversion of LC3-I to LC3-II (autophagy markers) between 12hours and 48 hours, confirms the inhibitory effects on autophagy.3-Methyladenine induces cell death is independent of autophagy inhibition.3-Methyladenine significantly shortens the duration of nocodazole-induced-prometaphase arrest.(In Vivo):3-Methyladenine (1.5?mg/100?g; intraperitoneal injection; 3-24?hours) treatment alleviates sodium taurocholate-induced severe acute pancreatitis (SAP) in rats at both 12 hours and 24?hours.3-Methyladenine inhibits autophagy of pancreatic acinar cells in sodium taurocholate-tnduced SAP.3-Methyladenine also shows inhibitory effects on PI3K/Akt signaling pathway and NF-κB signaling pathway in sodium taurocholate-induced SAP.

Cell Viability Assay Cell Line:HeLa cells Concentration:0 mM, 2.5 mM or 5 mM, 10 mMIncubation Time:0 hour, 24 hours and 48 hours Result:Decreased cell viability in a time-and dose-dependent manner, and was associated with caspase-3 activation.Cell Autophagy Assay Cell Line:HeLa cells Concentration:5 mM Incubation Time:24 hours Result:Suppressed autophagy in HeLa cells under both glucose-free conditions and normal conditions.Western Blot Analysis Cell Line:HeLa cells Concentration:5 mM Incubation Time:0 hour, 12 hours, 24 hours and 48 hours Result:Suppressed conversion of LC3-I to LC3-II between 12 hours and 48 hours.

Animal Model:10–12 weeks Specific pathogen free- (SPF-) grade healthy male Sprague-Dawley (SD) rats (250–290?g)Dosage:1.5?mg/100?g (1000 μM) Administration:Intraperitoneal injection Result:Alleviated Sodium Taurocholate-Induced SAP.

3-MA

PI3K/Akt/mTOR signaling

PI3K

PI3Kγ|Vps34

Cancer

——

5142-23-4

149.1533

C6H7N5

>98% (HPLC)

DMSO: ≥ 1.5 mg/mL; DMSO: 6.8 mg/mL (Need ultrasonic); H2O: 8.82 mg/mL (Need ultrasonic)

NC(N=CN1C)=C2C1=NC=N2

3H-Purin-6-amine, 3-methyl-

(-20℃)

With Ice Pack

≥ 2 years