AICAR (Acadesine)

For research use only.

Catalog No.S1802 Synonyms: NSC105823

64 publications

AICAR (Acadesine) Chemical Structure

CAS No. 2627-69-2

AICAR (Acadesine, NSC105823), 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.

Size Price Stock Quantity  
EUR 49 In stock
EUR 167 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's AICAR (Acadesine) has been cited by 64 publications

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Description AICAR (Acadesine, NSC105823), 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.
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 MlfUSpVv[3Srb36gZZN{[Xl? MX:1NFAh|ryP NXftNld[PSCq NF:5OVdC[3SrdnH0bY9vKG:oIFHNVGshcW5ibX;1d4UhO1R|TEGgZ4VtdHNiYYPz[ZN{\WRiYYOgRW1RUyCyaH;zdIhwenmuYYTpc44h[XRiNUCwJJVOKGGodHXyJFUhcHK|IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYO= MkH5NlUzPjJ7NEC=
mouse 3T3L1 cells MoG4SpVv[3Srb36gZZN{[Xl? MoG0NE4zKG2P NWrsNGFkQSCmYYnz Ml\iTY5kemWjc3WgbY4hSU2SS3HsdIhiKFSqckG3NkBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiMD6yJI1OKGGodHXyJFkh\GG7czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MVyyOlA5QDN|NR?=

... 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
  • 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
Smiles C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

AMPK Signaling Pathway Map

Related AMPK Products

  • HTH-01-015 New

    HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy.

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.

  • Phenformin HCl

    Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

  • A-769662

    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

  • Dorsomorphin (Compound C) 2HCl

    Dorsomorphin 2HCl (BML-275, Compound C) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.

  • WZ4003

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus, AY 22989, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

  • MK-2206 2HCl

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • CHIR-99021 (CT99021) HCl

    CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.

Tags: buy AICAR (Acadesine) | AICAR (Acadesine) supplier | purchase AICAR (Acadesine) | AICAR (Acadesine) cost | AICAR (Acadesine) manufacturer | order AICAR (Acadesine) | AICAR (Acadesine) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID