Meriolin 3

A cell-permeable, ATP site-targeting azaindolopyrimidine compound that is reported to inhibit the kinase activity of CDK9/cyclin T, CDK2/cyclin A, CDK1/cyclin B, CDK5/p25 (IC₅₀ = 6, 11, 170, 170 nM, respectively), DYRK1A, CKIδ/ε, GSK-3α/β (IC₅₀ = 29, 200, and 230 nM, respectively), as well as CDK3/cyclin E, CDK4/cyclin D1, CDK6/cyclin D1, CDK7/cyclin H, and FLT3 (IC₅₀<400 nM), while showing much reduced activity agasint 21 other kinases (IC₅₀ >1 µM). Shown to effectively inhibit cellular CDK substrates phosphorylation and induce apoptosis in SH-SY5Y neuroblastoma cultures (Effective conc. 0.3 to 1 µM) in vitro and retard A4573- and LS174T-derived tumor growths in mice in vivo (1 to 5 mg/kg/day, i.p.). Cell viability tests reveal that Meriolin 3 selectively affects the viability of a panel of 8 cancer lines (IC₅₀ ≤380 nM) in comparison to normal human foreskin fibroblasts (IC₅₀ = 8 µM).

Packaged under inert gas

Toxicity: Regulatory Review (Z)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Echalier, A., et al. 2008. J. Med. Chem.51, 737.
Bettayeb, K., et al. 2007. Cancer Res.67, 8325.

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