Home	Quick Product Lists	Contact LC Labs	Login/Register	My Account	View Cart
In Business 29 Years - Since 1980		THE CURRENT TIME at LC Labs is:

K-2151 K252a, >99%

[K-252a]

M.W. 467.47

C27H21N3O5

[97161-97-2]

[99533-80-9]

RTECS NZ0550000

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

Find and View a Certificate of Analysis for this product

View the MSDS for this product

• 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, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.