3-Methyladenine

SKU: orb1224859

Description

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.

Key Properties

• CAS Number: 5142-23-4
• MW: 149.1533
• Purity: >98% (HPLC)
• Formula: C₆H₇N₅
• SMILES: NC(N=CN1C)=C2C1=NC=N2
• Target: PI3K
• Solubility: DMSO: ≥ 1.5 mg/mL; DMSO: 6.8 mg/mL (Need ultrasonic); H2O: 8.82 mg/mL (Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  Cell Viability Assay Cell line: HeLa cells. Concentration: 0 mM, 2.5 mM or 5 mM, 10 mM Incubation 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

3-MA

Quick Database Links

Gene Symbol

PI3K