Background
Originally isolated from the soil fungi Nocardiopisis sp., K252a is a staurosporine analog that inhibits various protein kinases through competition with the ATP binding site (1,2). K252a is a reversible cell-permeable, potent inhibitor of phosphorylase kinase (IC50 = 1.7 nM), protein kinase A (PKA) (IC50 = 140 nM), and protein kinase C (PKC) (IC50 = 470 nM) (3,4). K252a is also known to inhibit protein kinase G and CaM kinase II (5,6). K252a inhibits nerve growth factor induced Trk activation (IC50 = 3 nM), as well as downstream signaling (5,7,8). K252a is reported to induce apoptosis and cell cycle arrest through cdc25 and cdc2 inhibition (9).
- Kase, H. et al. (1986) J Antibiot (Tokyo) 39, 1059-65.
- Kase, H. et al. (1987) Biochem Biophys Res Commun 142, 436-40.
- Elliott, L.H. et al. (1990) Biochem Biophys Res Commun 171, 148-54.
- Davis, P.D. et al. (1992) J Med Chem 35, 177-84.
- Koizumi, S. et al. (1988) J Neurosci 8, 715-21.
- Hashimoto, Y. et al. (1991) Biochem Biophys Res Commun 181, 423-9.
- Berg, M.M. et al. (1992) J Biol Chem 267, 13-6.
- Tapley, P. et al. (1992) Oncogene 7, 371-81.
- Chin, L.S. et al. (1999) Cancer Invest 17, 391-5.
Molecular Formula
C27H21N3O5
Molecular Weight
467.47 g/mol
Purity
>99%
CAS
99533-80-9
Solubility
Soluble in DMSO at 100mg/ml.
Storage
Directions for Use
K252a is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 100 μg in 213.9 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-1 µM for 0.5-1 hr prior to treating with a stimulator. Soluble in DMSO at 100 mg/ml; poorly soluble in ethanol.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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