K252a is an alkaloid isolated from Nocardiopsisbacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).[2][3][4][5][6][7][8][9]
K252a is reported to promote myogenic differentiation in C2 mouse myoblasts[6] and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.[10]
K252a has been reported in preclinical research as a potential treatment for psoriasis[11]
K252a inhibits tyrosine phosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252a.
k252a, alkaloid, isolated, from, nocardiopsis, bacteria, this, staurosporine, analog, highly, potent, cell, permeable, inhibitor, kinase, phosphorylase, kinase, ic50, nmol, respectively, higher, concentrations, also, efficient, inhibitor, serine, threonine, pr. K252a is an alkaloid isolated from Nocardiopsis bacteria This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase IC50 1 8 and 1 7 nmol L respectively At higher concentrations it is also an efficient inhibitor of serine threonine protein kinases IC50 of 10 to 30 nmol L 2 3 4 5 6 7 8 9 K252a NamesPreferred IUPAC name Methyl 13S 14R 16R 14 hydroxy 13 methyl 5 oxo 6 7 13 14 15 16 hexahydro 5H 13 16 epoxydiindolo 1 2 3 fg 3 2 1 kl pyrrolo 3 4 i 1 6 benzodiazocine 14 carboxylateIdentifiersCAS Number 99533 80 9 NChEMBL ChEMBL281948 NChemSpider 2299962 NECHA InfoCard 100 167 781IUPHAR BPS 336PubChem CID 3035817UNII IV7H45AM5B YCompTox Dashboard EPA DTXSID40880065InChI InChI 1S C27H21N3O5 c1 26 27 33 25 32 34 2 11 18 35 26 29 16 9 5 3 7 13 16 20 21 15 12 28 24 21 31 19 14 8 4 6 10 17 14 30 26 23 19 22 20 29 h3 10 18 33H 11 12H2 1 2H3 H 28 31 t18 26 27 m1 s1 YKey KOZFSFOOLUUIGY CYBHFKQVSA N YProperties 1 Chemical formula C 27H 21N 3O 5Molar mass 467 481 g mol 1Solubility in other solvents Soluble in DMSO dichloromethane and methanolExcept where otherwise noted data are given for materials in their standard state at 25 C 77 F 100 kPa N verify what is Y N Infobox references K252a is reported to promote myogenic differentiation in C2 mouse myoblasts 6 and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity 10 K252a has been reported in preclinical research as a potential treatment for psoriasis 11 K252a inhibits tyrosine phosphorylation of Trk A induced by NGF PC12 cells were incubated in the presence or absence of 10 ng ml NGF with or without various concentrations of K252a See also editK252b Lestaurtinib ANA 12 Cyclotraxin BReferences edit K252a from Fermentek Ruegg U T et al 1989 Tips 10 218 Eliot L H et al 1990 B B R C 171 148 Simpson D l et al 1991 J Neurosci Res 28 148 Chin L S et al 1999 Cancer Invest 17 391 a b Tapley P et al 1992 Oncogene 7 371 Hashimoto S 1998 J Cell Biol 107 1531 Kase H et al 1987 B B R C 142 436 Hirayama E et al 2001 B B R C 285 1237 Borasio G D Neurosci Lett 1990 108 207 Promising New Treatments for Psoriasis Sarah Dubois Declercq and Roxane Pouliot gt The Scientific World Journal Volume 2013 Article ID 980419 https dx doi org 10 1155 2013 980419Further reading editWood JL Stoltz BM Dietrich HJ 1995 Total synthesis of and K252a J Am Chem Soc 117 41 10413 4 doi 10 1021 ja00146a039 nbsp This biochemistry article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title K252a amp oldid 1213661109, wikipedia, wiki, book, books, library,
