AICAR (Acadesine)

Catalog No.S1802 Batch:S180213

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Technical Data

Formula

C9H14N4O5
Molecular Weight 258.23 CAS No. 2627-69-2
Solubility (25°C)* In vitro DMSO 52 mg/mL (201.37 mM)
Water 26 mg/mL (100.68 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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. AICAR (Acadesine) induces mitophagy. Phase 3.
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]
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]
Features A potential first-in-class adenosine regulating agent (ARA).

Protocol (from reference)

Cell Assay:

[3]
  • 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.
Animal Study:

[3]
  • Animal Models

    mouse xenograft model of K562 cells

  • Dosages

    50 mg/kg

  • Administration

    Injected intraperitoneally

Customer Product Validation

, , British Journal of Pharmacology, 2015, 172(13):3284–3301.

, , J Appl Toxicol, 2017, 37(10):1219-1224

Data from [Data independently produced by , , J Clin Invest, 2019, 129(1):252-267]

Data from [Data independently produced by , , J Mol Cell Cardiol, 2015, 85:155-67]

Selleck's AICAR (Acadesine) has been cited by 152 publications

Molecular mechanism underlying miR-204-5p regulation of adipose-derived stem cells differentiation into cells from three germ layers [ Cell Death Discov, 2024, 10(1):95] PubMed: 38388551
Forchlorfenuron-Induced Mitochondrial Respiration Inhibition and Metabolic Shifts in Endometrial Cancer [ Cancers (Basel), 2024, 16(5)976] PubMed: 38473335
Rap1GAP exacerbates myocardial infarction by regulating the AMPK/SIRT1/NF-κB signaling pathway [ Cell Signal, 2024, 117:111080] PubMed: 38320624
Maternal aging increases offspring adult body size via transmission of donut-shaped mitochondria [ Cell Res, 2023, 33(11):821-834] PubMed: 37500768
Enhanced glycolysis-mediated energy production in alveolar stem cells is required for alveolar regeneration [ Cell Stem Cell, 2023, 30(8):1028-1042.e7] PubMed: 37541209
ADP-dependent glucokinase controls metabolic fitness in prostate cancer progression [ Mil Med Res, 2023, 10(1):64] PubMed: 38082365
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] PubMed: 37649137
Gasdermin D-mediated pyroptosis is regulated by AMPK-mediated phosphorylation in tumor cells [ Cell Death Dis, 2023, 14(7):469] PubMed: 37495617
Gasdermin D-mediated pyroptosis is regulated by AMPK-mediated phosphorylation in tumor cells [ Cell Death Dis, 2023, 14(7):469] PubMed: 37495617

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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