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Chemical Structure| 5142-23-4 Chemical Structure| 5142-23-4

Structure of 3-Methyladenine
CAS No.: 5142-23-4

Chemical Structure| 5142-23-4

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3-Methyladenine is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM.

Synonyms: 3-MA; NSC 66389; 3-Methyladenine, NSC 66389

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Product Details of 3-Methyladenine

CAS No. :5142-23-4
Formula : C6H7N5
M.W : 149.15
SMILES Code : NC1=C2N=CN=C2N(C)C=N1
Synonyms :
3-MA; NSC 66389; 3-Methyladenine, NSC 66389
MDL No. :MFCD00010531
InChI Key :ZPBYVFQJHWLTFB-UHFFFAOYSA-N
Pubchem ID :135398661

Safety of 3-Methyladenine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of 3-Methyladenine

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:60 μM

  • Vps34

    Vps34, IC50:25 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
THLE2 cells 5 mM 6 h To inhibit autophagy and study the protective role of YAP in hepatic ischemia-reperfusion injury. Results showed that inhibition of autophagy weakened YAP-mediated cell protection, accompanied by a significant upregulation of apoptosis levels. Chin Med J (Engl). 2024 Mar 20;137(6):657-668.
mouse primary cortical neurons 5 mM 24 h To inhibit autophagy and evaluate its effect on neuronal survival. Results showed that 3-MA at appropriate concentrations significantly increased neuronal survival after oxygen-glucose deprivation (OGD). J Extracell Vesicles. 2020 Oct;10(1):e12024.
COV434 cells 5 mM 24 h Inhibited autophagy but did not significantly alleviate CDDP-induced ER stress and apoptosis Reprod Biol Endocrinol. 2018 Sep 3;16(1):85.
KGN cells 5 mM 24 h Inhibited autophagy but did not significantly alleviate CDDP-induced ER stress and apoptosis Reprod Biol Endocrinol. 2018 Sep 3;16(1):85.
cardiomyocytes 10 mM 3 h inhibited autophagy, significantly attenuated or ablated lethal toxin-induced cardiomyocyte contractile anomalies BMC Med. 2012 Nov 7;10:134.
osteoclasts 0.5 mM 72 h 3-MA reversed the enhanced autophagy levels by DOX, indicating that enhanced autophagy was responsible for the effects of DOX. Antioxidants (Basel). 2022 Jul 28;11(8):1476.
HEK293T cells 5 mg/mL 8 h To investigate the effect of 3-MA on BinCARD1 degradation, it was found that 3-MA inhibited TBK1-mediated autophagic degradation of BinCARD1. Cell Mol Immunol. 2022 Oct;19(10):1168-1184.
Newborn mouse ovarian cells 1 mM 3 days Inhibited autophagy, leading to a decreased percentage of primordial follicles Cell Death Dis. 2020 Sep 10;11(9):737.
Mouse embryonic fibroblasts (MEFs) 5 mM Inhibition of autophagy, leading to increased toxicity in glucose-starved wild-type MEFs, similar to the effect of RelA inactivation. Nat Cell Biol. 2011 Aug 28;13(10):1272-9.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Hepatic ischemia-reperfusion injury model Intraperitoneal injection 15 mg/kg Once, 1 hour before I/R model establishment To inhibit autophagy and study the protective role of YAP in hepatic ischemia-reperfusion injury. Results showed that inhibition of autophagy weakened YAP-mediated liver protection, accompanied by a significant upregulation of apoptosis levels. Chin Med J (Engl). 2024 Mar 20;137(6):657-668.
C57BL/6 male mice Transverse aortic constriction (TAC)-induced cardiac hypertrophy model Intraperitoneal injection 20 mg/kg Once daily for 4 weeks 3-MA inhibited PKD siRNA-induced increase in autophagy and prevented the ameliorative effects of PKD siRNA on cardiac hypertrophy Int J Biol Sci. 2017 Feb 12;13(3):276-285
C57BL/6 mice Middle cerebral artery occlusion (MCAO) model Intraperitoneal injection 15 mg/kg Single injection at the beginning of reperfusion or 12 hours later To evaluate the inhibitory effect of 3-MA on autophagy after cerebral ischemia and its impact on neuroprotection and neurological recovery. Results showed that 3-MA injection at 12 hours after reperfusion significantly reduced brain injury and improved neurological recovery. J Extracell Vesicles. 2020 Oct;10(1):e12024.
C57BL/6J mice Cisplatin-induced premature ovarian insufficiency model Intraperitoneal injection 10 mg/kg Consecutively for 7 days Inhibiting autophagy did not significantly alleviate CDDP-induced ovarian damage and hormone dysregulation Reprod Biol Endocrinol. 2018 Sep 3;16(1):85.
Mice TAC-induced heart failure model Intraperitoneal injection 15 mg/kg Every 3 days To inhibit autophagic induction and evaluate its effect on TAC-induced heart failure JACC Basic Transl Sci. 2023 Jul 19;8(9):1215-1239
C57BL/6J female mice DOX-induced bone loss model Intraperitoneal injection 5 mg/kg DOX once per week for three weeks; 3-MA daily for four weeks Injection of 3-MA reversed DOX-induced bone loss and reduced the area of OCs on the bone surface. Antioxidants (Basel). 2022 Jul 28;11(8):1476.
Mice Heterotopic transplant model of intestinal fibrosis Intraperitoneal injection 10 mg/kg Once daily for 7 days 3-MA further inhibited autophagy in the grafted tissue and aggravated fibrosis. Cells. 2019 Sep 13;8(9):1078
BALB/C nude mice A2780 tumor xenograft model Not specified 5 mg/kg 3 weeks To investigate the effect of 3-MA on A2780 tumor growth, it was found that 3-MA could completely suppress autophagy induced by the combination of erlotinib and AZD2281 and attenuate its antitumor activity. Drug Des Devel Ther. 2015 Jun 22;9:3183-90

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.70mL

1.34mL

0.67mL

33.52mL

6.70mL

3.35mL

67.05mL

13.41mL

6.70mL

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