AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

Autophagy (rat hepatocytes):0.3 mM

METHODS: CCRF-CEM, HeLa, and L1210 cells were treated with different concentrations of AICAR for 3 days. particle counting analysis was used to evaluate the inhibition of cell growth.
RESULTS: AICAR inhibited the growth of CCRF-CEM cells (IC50=210 μM) and HeLa cells (IC50=165 μM), but did not inhibit the growth of L1210 cells (IC50≥ 250 μM). [1]
METHODS: HCT-116 and HEK293 cells were treated with AICAR for 48 hours, and cytotoxicity was detected by the MTT method.
RESULTS: AICAR is non-toxic to HCT-116 (EC50> 100 μM) and HEK293 (EC50> 100 μM) cells. [2]
METHODS: K562 and K-562R cells were treated with AICAR for 48 hours, and the cytotoxicity was detected by the XTT method.
RESULTS: AICAR showed cytotoxicity to K562 (IC50=800 μM) and K-562R (IC50=800 μM). [3]
METHODS: K562 cells were treated with AICAR for 48 hours, and the anti-leukemia activity was detected by the XTT method.
RESULTS: AICAR exhibited anti-leukemia activity against K562 (IC50=800 μM). [4]
METHODS: MDA-MB-231 and RCC4 cells were treated with AICAR for 48 hours, and the anti-tumor activity was detected by the XTT method.
RESULTS: AICAR exhibited anti-tumor activity against MDA-MB-231 cells (IC50=1000 μM) and RCC4 cells (IC50=250 μM). [5]
METHODS: MDA-MB-453 and SK-BR-3 cells were treated with AICAR for 4 days, and their antiproliferative activity was detected by the Celltiter-glo luminescent cell viability assay.
RESULTS: AICAR exhibited anti-tumor activity against MDA-MB-453 cells (IC50=1700 μM) and SK-BR-3 cells (IC50=180 μM). [6]
METHODS: HepG2 cells were treated with AICAR (0.1-1.0 mM) for 12, 24 and 48 hours, and the protein levels were detected by western blot.
RESULTS: The expression levels of IR-β in 0.25, 0.5 and 1.0 mM AICAR significantly decreased to 50%, 53% and 46% of the control at 48 h. [7]

METHODS: To study the anti-tumor activity of AICAR, AICAR was subcutaneously injected (300 mg/kg/ day) into xenograft tumor mice derived from the H1975 cell line.
RESULTS: AICAR significantly inhibited tumor growth, and the tumor weight decreased by 47% (p<0.05). The expression level of Ki-67 in tumor tissues treated with AICAR decreased, indicating a reduction in cell proliferation, while the expression levels of DNA damage markers γ-H2AX and p21Cip1 increased. [8]
METHODS: To study the anti-tumor activity of AICAR, xenograft mice of MG63 and KHOS osteosarcoma cell lines were administered with AICAR (450 mg/kg/ day).
RESULTS: AICAR treatment significantly inhibited tumor growth, and the tumor volume decreased by 14.1% and 35.4% respectively (p<0.05). Mitochondrial proliferation and apoptotic activities increased in tumor tissues treated with AICAR. [9]

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)