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K-252a

Protein kinase inhibitor
 
BML-EI152-0100 100 µg 130.00 USD
 
BML-EI152-1000 1 mg 521.00 USD
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Replaces Prod. #: ALX-380-027

Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Acts by binding to the ATP binding domain of the kinase. Potent inhibitor of Ca2+/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC) (Ki=25nM), trk tyrosine kinase family members (gp140trk; IC50 =3nM) and cGMP-dependent protein kinase (PKG). Binds with high affinity to neuroblastoma membrane (2.7nM), promoting survival of primary neuronal cultures (75nM) and induction of neurite outgrowth in SH-SY5Y neuroblastoma cells along with phosphorylation of pp125 focal adhesion protein tyrosine kinase. Induces apoptosis.

Product Specification

Formula:C27H21N3O5
 
MW:467.5
 
CAS:99533-80-9
 
RTECS:NZ0550000
 
Purity:≥98% (HPLC)
 
Appearance:Lyophilized solid.
 
Solubility:Soluble in DMSO (1mg/ml) or dimethyl formamide (1mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C.
 
Handling:Protect from light.
 
380-027
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380-027

Product Literature References

Self-amplified BDNF transcription is a regulatory system for synaptic maturation in cultured cortical neurons: S. Nakajima, et al. ; Neurochem. Int. 91, 55 (2015), Application(s): Cell culture , Abstract;
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review, Abstract;
K-252a induces tyrosine phosphorylation of the focal adhesion kinase and neurite outgrowth in human neuroblastoma SH-SY5Y cells: A.C. Maroney, et al.; J. Neurochem. 64, 540 (1995), Abstract;
K-252a promotes survival and choline acetyltransferase activity in striatal and basal forebrain neuronal cultures: M.A. Glicksman, et al.; J. Neurochem. 64, 1502 (1995), Abstract;
Membranes of human neuroblastoma SH-SY5Y cells contain specific binding sites for [3H]K-252A: E. Knight, et al.; Biochem. Biophys. Res. Commun. 211, 511 (1995), Abstract;
Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose: B. Cheng, et al.; J. Neurochem. 62, 1319 (1994), Abstract;
Ecto-protein kinase and surface protein phosphorylation in PC12 cells: interactions with nerve growth factor: Z. Pawlowska, et al.; J. Neurochem. 60, 678 (1993), Abstract;
K-252a and staurosporine promote choline acetyltransferase activity in rat spinal cord cultures: M.C. Glicksman, et al.; J. Neurochem. 61, 210 (1993), Abstract;
Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC: K. Mizuno, et al.; FEBS Lett. 330, 114 (1993), Abstract;
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992), Abstract;
K-252a and staurosporine selectively block autophosphorylation of neurotrophin receptors and neurotrophin-mediated responses: S.H. Nye, et al.; Mol. Biol. Cell 3, 677 (1992), Abstract;
K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity: M.M. Berg, et al.; J. Biol. Chem. 267, 13 (1992), Abstract; Full Text
K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors: P. Tapley, et al.; Oncogene 7, 371 (1992), Abstract;
pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells: E.D. Lloyd & M.W. Wooten; J. Neurochem. 59, 1099 (1992), Abstract;
Differentiation of PC12 cells with K-ras: comparison with nerve growth factor: D.L. Simpson, et al.; J. Neurosci. Res. 28, 486 (1991), Abstract;
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991), Abstract;
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990), Abstract;
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review), Abstract;
K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; Biochem. Biophys. Res. Commun. 142, 436 (1987), Abstract;
K252a, a new inhibitor of protein kinase C, concomitantly inhibits 40K protein phosphorylation and serotonin secretion in a phorbol ester-stimulated platelets: K. Yamada, et al.; Biochem. Biophys. Res. Commun. 144, 35 (1987), Abstract;
K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986), Abstract;
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. (Tokyo) 39, 1072 (1986), Abstract;

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