K-2151 K252a, >99%

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  • 5 mg
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  • 60
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  • 10 mg
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  • 110
  • 97
  • 15,600
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  • 25 mg
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  • 50 mg
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  • 338
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  • 100 mg
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  • 250 mg
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  • 1,099
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  • 500 mg
  • 1,780
  • 1,651
  • 1,456
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  • M.W. 467.47
  • C27H21N3O5
  • [97161-97-2]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; poorly soluble in ethanol. Disposal: A.

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  • K252a is a kinase inhibitor that inhibits PKA (Ki = 18 nM), PKC (Ki = 25 nM), and PKG (Ki = 20 nM). Kase, H., et al. "K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases." Biochem. Biophys. Res. Commun. 142: 436-440 (1987).
  • Potently inhibits CaMK (Ki = 1.8 nM), competitively with ATP and noncompetitively with the substrate. Hashimoto, Y., et al. "Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926." Biochem. Biophys. Res. Commun. 181: 423-429 (1991).
  • Potently inhibits phosphorylase kinase (IC50 = 1.7 nM), with 300-fold selectivity for this enzyme over protein kinase C. Elliott, L.H., et al. "K252a is a potent and selective inhibitor of phosphorylase kinase." Biochem. Biophys. Res. Commun. 171: 148-154 (1990).
  • Potent inhibitor of the tyrosine phosphorylation of p140prototrk; K252a also has a direct effect on the p140prototrk tyrosine kinase. Berg, M.M., et al. "K-252a Inhibits Nerve Growth Factor-induced trk Proto-oncogene Tyrosine Phosphorylation and Kinase Activity." J. Biol. Chem. 267: 13-16 (1992).
  • Potent inhibitor of pp42/44 MAP kinase in vitro and in vivo. Lloyd, E.D. and Wooten, M.W. "pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells." J. Neurochem. 59: 1099-1109 (1992).
  • K252a apparently induces apoptosis by suppressing phosphorylation of Rb, upregulating p21, and inhibiting Cdc2 and Cdc25c activity. Mohri, T., et al. "K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c." Cancer Invest. 17: 391-395 (1999).
  • Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
  • We note that one of our competitors, AG Scientific, as of February 11, 2014, is claiming 99.86% purity for its K252a. This claim is not credible in general chemical terms for this complex organic compound, nor in terms of the sensitivity and reproducibility of generally utilized analytical techniques.
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