AICAR (Acadesine)

Catalog No.S1802 Synonyms: NSC105823, AICA Riboside

For research use only.

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

CAS No. 2627-69-2

Selleck's AICAR (Acadesine) has been cited by 102 publications

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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.
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
3T3L1 M1rHcmZ2dmO2aX;uJIF{e2G7 NYPlNZZnOC5{IH3N M2exN|kh\GG7cx?= M4\0UGlv[3KnYYPlJIlvKEGPUFvhcJBp[SCWaIKxO|IheGixc4Doc5J6dGG2aX;uJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG2IECuNkBuVSCjZoTldkA6KGSjeYOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NV24U5V4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFg{OzVpPkK2NFg5OzN3PD;hQi=>
3T3L1 M3P1[mZ2dmO2aX;uJIF{e2G7 M2TEfFUxOCEQvF2= MVW1JIg> NHHhSWFC[3SrdnH0bY9vKG:oIFHNVGshcW5ibX;1d4UhO1R|TEGgZ4VtdHNiYYPz[ZN{\WRiYYOgRW1RUyCyaH;zdIhwenmuYYTpc44h[XRiNUCwJJVOKGGodHXyJFUhcHK|IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYO= MnSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NkK5OFAoRjJ3Mk[yPVQxRC:jPh?=
C2C12 MWnGeY5kfGmxbjDhd5NigQ>? MYixJI1O MoK5NUBpeg>? NILQUXNC[3SrdnH0bY9vKG:oIFHNVGshcW5ibX;1d4UhSzKFMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hSUOFIIDoc5NxcG:{eXzheIlwdiCjdDDT[ZI4QSC{ZYPp[JVmeyCjdDCxJI1OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NF7CVIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{i4O|g1PCd-Mke4PFc5PDR:L3G+
3T3L1 NYW4T5NvTnWwY4Tpc44h[XO|YYm= NITvdpEzKG2P NYOwTG16PCCqcoO= MoC1TY5lfWO2aX;uJI9nKEGPUFvhcJBp[SCyaH;zdIhwenmuYYTpc44h[XRiVHjyNVczKHKnc3nkeYUhcW5ibX;1d4UhO1R|TEGgZ4VtdHNiYYSgNkBuVSCjZoTldkA1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M2KwdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEK1PFE4Lz5{OUSyOVgyPzxxYU6=
C2C12 NHnvUXNHfW6ldHnvckBie3OjeR?= NXS1O|h2OC5{IH3N M{\pS|MxKG2rboO= MU\Jcohq[mm2aX;uJI9nKFCWUEHCJIlvKGSrZn\ldoVvfGmjdHXkJI1wfXOnIFOyR|EzKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBCS0NicHjvd5Bpd3K7bHH0bY9vKGG2IGPldk04QSC{ZYPp[JVmKGG2IECuNkBuVSCjZoTldkA{OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhd5NigQ>? NH7o[YU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1NVA4QSd-Mki5OVExPzl:L3G+
RCC4 NFLkZllHfW6ldHnvckBie3OjeR?= NIHzXIQyKG2P NG\yeoY1QCCqcoO= NVH4fIF1UW6mdXP0bY9vKG:oIHH1eI9xcGGpeTDpckBpfW2jbjDSR2M1KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIFzDN{Bkd264ZYLzbY9vKGG2IEGgcW0h[W[2ZYKgOFghcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> M1nYcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{K1OlAxLz5{OEOyOVYxODxxYU6=
3T3L1 MXzGeY5kfGmxbjDhd5NigQ>? NUDrcWVGOC5{IH3N M{W3eWlvcGmkaYTpc44hd2ZiYXTpdI9o\W6nc3nzJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckB1emmpbInj[ZJq\GViY3;ueIVvfCCjdDCwMlIhdU1iYomgZ49td3KrbXX0dolkKGG|c3H5 NVPjUmQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFg{OzVpPkK2NFg5OzN3PD;hQi=>
3T3L1 MWnGeY5kfGmxbjDhd5NigQ>? MlXpNE4zKG2P NXXSR4V1OyCmYYnz MUXS[YR2[3Srb36gbY4hW0OGMTDwdo91\WmwIHX4dJJme3Orb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiMD6yJI1OKGGodHXyJFMh\GG7czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6OEOzOUc,OjZyOEizN|U9N2F-
3T3L1 MVfGeY5kfGmxbjDhd5NigQ>? Mkn1NE4zKG2P MmDnN{Bl[Xm| MlrkVoVlfWO2aX;uJIlvKFOURVLQMVFkKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDtc5V{\SB|VEPMNUBk\WyuczDheEAxNjJibV2gZYZ1\XJiMzDkZZl{KGK7IGfld5Rmem5iYnzveEBu\XSqb3S= NF3ySXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4PFM{PSd-Mk[wPFg{OzV:L3G+
3T3L1 NYC5Z5h1TnWwY4Tpc44h[XO|YYm= MnXENE4zKG2P NEPTZoE6KGSjeYO= MnzLRYN1cX[jdHnvckBw\iCDTWDLJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJGFESyCVZYK3PUBxcG:|cHjvdplt[XSrb36gZZQhOC5{IH3NJIFnfGW{IEmg[IF6eyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k NUflU5NuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFg{OzVpPkK2NFg5OzN3PD;hQi=>
3T3L1 M2ryWWZ2dmO2aX;uJIF{e2G7 MY[wMlIhdU1? M1TqRlMh\GG7cx?= M3HmUHJm\HWldHnvckBqdiCFL1XCVIFteGijIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBud3W|ZTCzWFNNOSClZXzsd{BifCByLkKgcW0h[W[2ZYKgN{Bl[Xm|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> M{TM[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEi4N|M2Lz5{NkC4PFM{PTxxYU6=
3T3L1 MYnGeY5kfGmxbjDhd5NigQ>? M{TiZVAvOiCvTR?= NIPBdoc{KGSjeYO= MkjFVoVlfWO2aX;uJIlvKFCSQWLnZY1u[SCycn;0[YlvKGW6cILld5Nqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOC5{IH3NJIFnfGW{IEOg[IF6eyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k MknoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOEizN|UoRjJ4MEi4N|M2RC:jPh?=
3T3L1 NELtPWdHfW6ldHnvckBie3OjeR?= MX[wMlIhdU1? NUPnUY5IOyCmYYnz NF7UPZBT\WS3Y4Tpc44hcW5iRlHTJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCvb4Xz[UA{XDOOMTDj[YxteyCjdDCwMlIhdU1iYX\0[ZIhOyCmYYnzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6OEOzOUc,OjZyOEizN|U9N2F-
Assay
Methods Test Index PMID
Western blot Cyclin D1 / p21 / p53 ; p-AMPK / p-ACC / p-eNOS / eNOS / vWF / VE-cadherin / ICAM-1 ; p-IRS-1 / IRS-1 / p-AKT / AKT ; p-S6K1 / S6K1 / p-ERK / ERK 19347029 18599796 26528831
Immunofluorescence YAZ / TAZ ; p-ERK 29730476 26528831
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 (from reference)

Cell Research:

[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 Research:

[3]

  • Animal Models: mouse xenograft model of K562 cells
  • Dosages: 50 mg/kg
  • Administration: Injected intraperitoneally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 258.23
Formula

C9H14N4O5

CAS No. 2627-69-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

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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

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