Home PI3K/Akt/mTOR AMPK activator - Mitophagy activator AICAR (Acadesine) For research use only.

AICAR (Acadesine)

Synonyms: NSC105823, AICA Riboside

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.

AICAR (Acadesine) Chemical Structure

AICAR (Acadesine) Chemical Structure

CAS: 2627-69-2

Selleck's AICAR (Acadesine) has been cited by 147 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Products often used together with AICAR (Acadesine)

Rituximab (anti-CD20)

Acadesine and Rituximab inhibits tumor outgrowth in the CB17-SCID mouse xenograft model of mantle cell lymphoma.

Montraveta A, et al. Oncotarget. 2014 Feb; 5(3): 726–739.

Tanespimycin (17-AAG)

AICAR and 17-AAG treatment reduces cell proliferation and affects chromosome segregation in MEFs and human cancer cells.

Tang YC, et al. Cell. 2011 Feb 18; 144(4): 499–512.

Venetoclax (ABT-199)

Acadesine and Venetoclax together are effective in inhibiting tumor growth in a mouse model of mantle cell lymphoma with high Bcl-2 expression.

Montraveta A, et al. Oncotarget. 2015 Aug 28;6(25):21159-72.

Nutlin-3a

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

Coll-Mulet L, et al. Blood. 2006 May 15;107(10):4109-14.

Metformin

Acadesine and Metformin as AMPK activators hinder miR-146a expression at the transcriptional level by promoting IκB kinase (IKK) phosphorylation to attenuate nuclear factor-kappaB (NF-κB) activity.

Gong H, et al. Signal Transduct Target Ther. 2022; 7: 66.

Other AMPK Products

Related compound libraries

Choose Selective AMPK Inhibitors

Cell Data

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

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.
Features A potential first-in-class adenosine regulating agent (ARA).
Targets
AMPK [1]
(Cell-free assay)		 AMPKK [1]
(Cell-free assay)
In vitro
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 Research 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.
Experimental Result Images 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 26528831
Immunofluorescence p-ERK YAZ / TAZ 26528831
In Vivo
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]
Animal Research Animal Models mouse xenograft model of K562 cells
Dosages 50 mg/kg
Administration Injected intraperitoneally

Chemical lnformation & Solubility

Molecular Weight 258.23 Formula

C9H14N4O5
CAS No. 2627-69-2 SDF Download AICAR (Acadesine) SDF
Smiles C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 51 mg/mL ( (197.49 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 20 mg/mL

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy AICAR (Acadesine) | AICAR (Acadesine) supplier | purchase AICAR (Acadesine) | AICAR (Acadesine) cost | AICAR (Acadesine) manufacturer | order AICAR (Acadesine) | AICAR (Acadesine) distributor