K-252b is a general, cell permeable protein kinase inhibitor which acts by binding to the ATP binding domain of the kinase. K-252b is a potent inhibitor of CaMKII (Ca2+/calmodulin kinase II), MYLK (myosin light chain kinase, Ki=0.147 μM), PKA (cAMP- dependent protein kinase, Ki=0.09 μM), PKC (protein kinase C, Ki=0.02 μM), and cGKI (cGMP-dependent protein kinase, Ki=0.1 μM).
1. Nakanishi, S., et al. 1986. J. Antibiot. 39: 1066-1071. PMID: 3759658 2. Kase, H., et al. 1987. Biochem. Biophys. Res. Commun. 142: 436-440. PMID: 3028414 3. Knüsel, B. and Hefti, F. 1991. J. Neurochem. 57: 955-962. PMID: 1861160 4. Teshima, R., et al. 1997. J. Immunol. 159: 964-969. PMID: 9218617 5. Pong, K., et al. 1997. J. Neurochem. 69: 986-994. PMID: 9282920 6. Fujii, S., et al. 2002. Neuroscience. 113: 617-628. PMID: 12150781
Soluble in DMSO (1 mg/ml), DMF (1 mg/ml), and methanol (2 mg/ml).
Store at -20° C
318.16° C (Predicted)
~769.8° C at 760 mmHg (Predicted)
~1.8 g/cm3 (Predicted)
Protein kinase C zeta: IC50 = 38 nM (Homo sapiens); Protein kinase C delta: IC50 = 38 nM (Homo sapiens); Protein kinase C eta: IC50 = 38 nM (Homo sapiens); Protein kinase C mu: IC50 = 38 nM (Homo sapiens); Protein kinase C gamma: IC50 = 38 nM (Homo sapiens); Protein kinase C beta: IC50 = 38 nM (Homo sapiens); Protein kinase C nu: IC50 = 38 nM (Homo sapiens); Protein kinase C alpha: IC50 = 38 nM (Homo sapiens); Protein kinase C theta: IC50 = 38 nM (Homo sapiens); Protein kinase C epsilon: IC50 = 38 nM (Homo sapiens); Protein kinase C iota: IC50 = 38 nM (Homo sapiens)
myosin light chain kinase(MLCK): Ki= 0.15 µM; cAMP- dependent protein kinase(PKA): Ki= 0.09 µM; protein kinase C(PKC): Ki= 0.02 µM; cGMP-dependent protein kinase(PKG): Ki= 0.1 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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