Home PI3K/Akt/mTOR AMPK activator - Mitophagy activator AICAR (Acadesine)

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AICAR (Acadesine) AMPK activator

Cat.No.S1802

AICAR (Acadesine, NSC105823, AICA Riboside), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. This compound induces mitophagy. Phase 3.
AICAR (Acadesine) AMPK activator Chemical Structure

Chemical Structure

Molecular Weight: 258.23

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Products Often Used Together with AICAR (Acadesine)

Tanespimycin (17-AAG)

Treatment with this compound and 17-AAG reduces cell proliferation and affects chromosome segregation in MEFs and human cancer cells.

Nutlin-3a

Nutlin-3a shows no synergistic activity with this compound as it induces p53-independent apoptosis.

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3L1 Function assay 0.2 mM 9 days Increase in AMPKalpha Thr172 phosphorylation in mouse 3T3L1 cells at 0.2 mM after 9 days by Western blot method 26088335
3T3L1 Function assay 500 μM 5 h Activation of AMPK in mouse 3T3L1 cells assessed as AMPK phosphorylation at 500 uM after 5 hrs by Western blotting analysis 25262940
C2C12 Function assay 1 mM 1 hr Activation of AMPK in mouse C2C12 cells assessed as increase in ACC phosphorylation at Ser79 residues at 1 mM after 1 hr by Western blot analysis 27887844
3T3L1 Function assay 2 mM 4 hrs Induction of AMPKalpha phosphorylation at Thr172 residue in mouse 3T3L1 cells at 2 mM after 4 hrs by Western blot analysis 29425817
C2C12 Function assay 0.2 mM 30 mins Inhibition of PTP1B in differentiated mouse C2C12 cells assessed as upregulation of ACC phosphorylation at Ser-79 residue at 0.2 mM after 30 mins by Western blot assay 28951079
RCC4 Function assay 1 mM 48 hrs Induction of autophagy in human RCC4 cells assessed as increase in LC3 conversion at 1 mM after 48 hrs by Western blot method 28325600
3T3L1 Function assay 0.2 mM Inhibition of adipogenesis in mouse 3T3L1 cells assessed as reduction in triglyceride content at 0.2 mM by colorimetric assay 26088335
3T3L1 Function assay 0.2 mM 3 days Reduction in SCD1 protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method 26088335
3T3L1 Function assay 0.2 mM 3 days Reduction in SREBP-1c protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method 26088335
3T3L1 Function assay 0.2 mM 9 days Activation of AMPK in mouse 3T3L1 cells assessed as increase in ACC Ser79 phosphorylation at 0.2 mM after 9 days by Western blot method 26088335
3T3L1 Function assay 0.2 mM 3 days Reduction in C/EBPalpha protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method 26088335
3T3L1 Function assay 0.2 mM 3 days Reduction in PPARgamma protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method 26088335
3T3L1 Function assay 0.2 mM 3 days Reduction in FAS protein expression in mouse 3T3L1 cells at 0.2 mM after 3 days by Western blot method 26088335
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 258.23 Formula

C9H14N4O5

 Storage (From the date of receipt)
CAS No. 2627-69-2 Download SDF Storage of Stock Solutions

Synonyms NSC105823, AICA Riboside Smiles C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N

Solubility

In vitro
Batch:

DMSO : 51 mg/mL (197.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 20 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Features
A potential first-in-class ARA.
Targets/IC50/Ki
AMPK [1]
(Cell-free assay)
AMPKK [1]
(Cell-free assay)
In vitro

Acadesine (500 μM) increases the ZMP content in extracts of isolated hepatocytes after up to 30-40 min treatment, then remains fairly constant at approximately 4 nmol/g. This compound causes a transient 12-fold activation of AMPK at 15 min in rat hepatocytes and 2-3 fold activation of AMPK in adipocytes, without affecting levels of ATP, ADP or AMP. It also causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes, as well as a dramatic inactivation of HMG-CoA reductase. [1] AICAR induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380 μM. At 0.5 mM, it decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%, and induces caspase activation and cytochrome c release from mitochondria. Uptake and phosphorylation of the compound are required to induce apoptosis and activate AMPK in B-CLL cells. While concentrations of 2-4 mM only slightly affect the viability of T cells from B-CLL patients, 0.5 mM remarkedly reduces viability of B cells but not T cells. [2] It triggers loss of cell metabolism in K562, LAMA-84 and JURL-MK1 and is also effective in killing resistant K562 cells and Ba/F3 cells carrying the T315I-BCR-ABL mutation. The effect of AICAR is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, it triggers relocation and activation of several PKC isoforms in K562 cells. The compound dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect is already detected at 0.25 mM and is maximal at 2.5 mM. [3] AICAR causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. [4] It significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood. [5]
In vivo

Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. [3] At 10 mg/kg, this compound results in higher fluid required to stabilize hemodynamics in pigs and inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation. [4]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8619186/
  • [5] https://pubmed.ncbi.nlm.nih.gov/7877305/

Applications

Methods Biomarkers Images PMID
Western blot p-S6K1 / S6K1 / p-ERK / ERK p-IRS-1 / IRS-1 / p-AKT / AKT p-AMPK / p-ACC / p-eNOS / eNOS / vWF / VE-cadherin / ICAM-1 Cyclin D1 / p21 / p53 S1802-WB1 26528831
Immunofluorescence p-ERK YAZ / TAZ S1802-IF1 26528831

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