AICAR (Acadesine)

Catalog No.S1802 Synonyms: NSC105823

AICAR (Acadesine) Chemical Structure

Molecular Weight(MW): 258.23

AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

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Cited by 37 Publications

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Biological Activity

Description AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.
Features A potential first-in-class adenosine regulating agent (ARA).
Targets
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. Acadesine (500 μM) 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. Acadesine (500 μM) causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes. Acadesine (500 μM) also causes a dramatic inactivation of HMG-CoA reductase. [1] Acadesine induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380 μM. Acadesine (0.5 mM) decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%. Acadesine (0.5 mM) induces caspase activation and cytochrome crelease from mitochondria. Uptake and phosphorylation of Acadesine (0.5 mM) are required to induce apoptosis and activate AMPK in B-CLL cells. Acadesine (2-4 mM) only slightly affects the viability of T cells from B-CLL patients, Acadesine (0.5 mM) remarkedly reduces viability of B cells but not T cells. [2] Acadesine triggers loss of cell metabolism in K562, LAMA-84 and JURL-MK1 and is also effective in killing imatinib-resistant K562 cells and Ba/F3 cells carrying the T315I-BCR-ABL mutation. The effect of Acadesine is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, Acadesine triggers relocation and activation of several PKC isoforms in K562 cells. Acadesine dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect of acadesine is already detected at 0.25 mM and is maximal at 2.5 mM. [3] Acadesine causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. [4] Acadesine significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood. [5]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse 3T3L1 cells NE\3ToJHfW6ldHnvckBie3OjeR?= NVrYRnZtPTByIN88US=> MmnwOUBp MUnBZ5RqfmG2aX;uJI9nKEGPUFugbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XO|ZYPz[YQh[XNiQV3QT{BxcG:|cHjvdplt[XSrb36gZZQhPTByIIXNJIFnfGW{IEWgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXN? MWCyOVI3Ojl2MB?=
mouse 3T3L1 cells NEjyeJlHfW6ldHnvckBie3OjeR?= NWfBWHZROC5{IH3N M2nJTVkh\GG7cx?= NX;lNXR[UW6lcnXhd4UhcW5iQV3QT4FteGijIGTodlE4OiCyaH;zdIhwenmuYYTpc44hcW5ibX;1d4UhO1R|TEGgZ4VtdHNiYYSgNE4zKG2PIHHmeIVzKDliZHH5d{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m Moq0NlYxQDh|M{W=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-S6K1 / S6K1 / p-ERK / ERK ; 

PubMed: 26528831     


BON cells were plated in 6-well plates and grown for 48 hours. Cells were treated with various doses of AICAR (left panel) or 1mM AICAR in the presence or absence of CC (10μM) (right panel) for 3 hours and lysed for Western blotting.

p-IRS-1 / IRS-1 / p-AKT / AKT ; 

PubMed: 26528831     


BON cells were plated in 6-well plates and grown for 48 hours. Cells were treated with various doses of AICAR for 3 hours and lysed for Western blotting.

p-AMPK / p-ACC / p-eNOS / eNOS / vWF / VE-cadherin / ICAM-1; 

PubMed: 18599796     


EPCs were treated with various concentrations of AICAR for 90 min.

Cyclin D1 / p21 / p53 ; 

PubMed: 19347029     

26528831 18599796 19347029
Immunofluorescence
p-ERK; 

PubMed: 26528831     


BON cells were plated on coverslips in 24-well plate and grown for 72 hours. Cells were treated as in A (right panel), and IF staining using p-ERK1/2 antibody and confocal microscopic analysis were performed. 

YAZ / TAZ ; 

PubMed: 29730476     


Representative microphotographs of control RPE-1 cells (Ctrl) and of the same cells stimulated with AICAR for 4 h or 24 h. DAPI (blue) was used to stain cell nuclei. Scale bars: 10 μm.

26528831 29730476
In vivo Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. [3] Acadesine (10 mg/kg) results in higher fluid required to stabilize hemodynamics in pigs. Acadesine (10 mg/kg) inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation in pigs. [4]

Protocol

Cell Research:

[3]
- Collapse
  • Cell lines: K562 cell lines
  • Concentrations: 2.5 mM
  • Incubation Time: 10 days
  • Method:

    Acadesine is added to K562 cell lines or primary cells (103 CD34+ cells/mL) growing in semisolid methyl cellulose medium. MethoCult H4100 or H4236 are used for cell lines and primary CD34+ cells respectively. Colonies are detected after 10 days of culture by adding 1 mg/mL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reagent and are scored by Image J quantification software.


    (Only for Reference)
Animal Research:

[3]
- Collapse
  • Animal Models: mouse xenograft model of K562 cells
  • Formulation: 0.9% NaCl
  • Dosages: 50 mg/kg
  • Administration: Injected intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 51 mg/mL (197.49 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing. 		6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 258.23
Formula

C9H14N4O5
CAS No. 2627-69-2
Storage powder
in solvent
Synonyms NSC105823

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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID