Highly potent inhibitor of protein and CAM kinases
Biological descriptionHighly potent, cell-permeable inhibitor of protein kinases such as PKA, PKC, PKG (IC50 = 18-25 nM), Serine/threonine protein kinases (IC50 values are 10-20 nM) and CAM kinase II (Ki = 1.8 nM). Analog of staurosporine (ab120056), exhibits a wide range of effects including neuroprotection and improvement of psoriasis in vivo.
Chemical name(9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 25 mM and in ethanol to 5 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Pan J et al. K252a prevents nigral dopaminergic cell death induced by 6-hydroxydopamine through inhibition of both mixed-lineage kinase 3/c-Jun NH2-terminal kinase 3 (JNK3) and apoptosis-inducing kinase 1/JNK3 signaling pathways. Mol Pharmacol72:1607-18 (2007).
Read more (PubMed: 17855652) »
Raychaudhuri SP et al. K252a, a high-affinity nerve growth factor receptor blocker, improves psoriasis: an in vivo study using the severe combined immunodeficient mouse-human skin model. J Invest Dermatol122:812-9 (2004).
Read more (PubMed: 15086569) »
Hashimoto Y et al. Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926. Biochem Biophys Res Commun181:423-9 (1991).
Read more (PubMed: 1659814) »
Kase H et al. K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochem Biophys Res Commun142:436-40 (1987).
Read more (PubMed: 3028414) »