AICAR (Acadesine)

Catalog No.S1802 Batch:S180212

Print

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 (warmed with 50ºC water bath) 23 mg/mL (89.06 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 30.000mg/ml (116.18mM) Taking the 1 mL working solution as an example, add 100 μL of 300 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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. This compound 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. 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]
Features A potential first-in-class ARA.

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    K562 cell lines

  • Concentrations

    2.5 mM

  • Incubation Time

    10 days

  • Method

    AICAR (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 the 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

References

  • https://pubmed.ncbi.nlm.nih.gov/7744080/
  • https://pubmed.ncbi.nlm.nih.gov/12522004/
  • https://pubmed.ncbi.nlm.nih.gov/19924252/
  • https://pubmed.ncbi.nlm.nih.gov/8619186/
  • https://pubmed.ncbi.nlm.nih.gov/7877305/

Customer Product Validation

<p>Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. *P < 0.05, **P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4).</p>

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

<p>Activation of AMPK with AICAR reduced INH-caused inhibition of mitochondrial biogenesis by activation of SIRT1-PGC1α pathway. HepG2 cells were exposed to INH (60mM) for 24 h in the presence or absence of an AMPK activator AICAR (0.095 mM). Expressions of PGC1α, NRF1 and COX IV (B) were analyzed by western blotting.</p>

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

(E) LDLR blocks the translocation of ALDH2 even AMPK activation. Scale bars: 5 μm.

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

Hela cells were pretreated with metformin (10 mM), AICAR (1 mM) and A769662 (100 μM)or vehicle (DMSO, 1:1000) 1 h prior to CVB3 infection. Cells were incubated for 12 h with indicated compound after viral infection. And cell lysates were subjected to western blot (A).

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

Selleck's AICAR (Acadesine) Has Been Cited by 169 Publications

CD137L promotes immune surveillance in melanoma via HLTF regulation [ Nat Commun, 2025, 16(1):8478] PubMed: 41006211
Calcium dysregulation disrupts mitochondrial homeostasis by interfering AMPK/Drp1 pathway to aggravate plaque progression and instability [ Theranostics, 2025, 15(15):7567-7583] PubMed: 40756371
Hypothalamic Astrocytes Exhibit Glycolytic Features Making Them Prone for Glucose Sensing [ Glia, 2025, 73(11):2253-2272] PubMed: 40708167
Knockdown of POLG Mimics the Neuronal Pathology of Polymerase-γ Spectrum Disorders in Human Neurons [ Cells, 2025, 14(7)480] PubMed: 40214434
Suppression of Fibroblast Growth Factor 23 in UMR106 Osteoblast-Like Cells and MC3T3-E1 Cells by Adipokine Chemerin [ Cell Biochem Funct, 2025, 43(2):e70051] PubMed: 39887469
Nuclear PD-L1 compartmentalization suppresses tumorigenesis and overcomes immunocheckpoint therapy resistance in mice via histone macroH2A1 [ J Clin Invest, 2024, 134(22)e181314] PubMed: 39545415
PRMT5 mediated FUBP1 methylation accelerates prostate cancer progression [ J Clin Invest, 2024, e175023] PubMed: 39146021
Brain Short-Chain Fatty Acids Induce ACSS2 to Ameliorate Depressive-Like Behavior via PPARγ-TPH2 Axis [ Research (Wash D C), 2024, 7:0400] PubMed: 38939042
Aerobic exercise suppresses CCN2 secretion from senescent muscle stem cells and boosts muscle regeneration in aged mice [ J Cachexia Sarcopenia Muscle, 2024, 15(5):1733-1749] PubMed: 38925632
Metabolic regulation of misfolded protein import into mitochondria [ Elife, 2024, 12RP87518] PubMed: 38900507

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.