-K252a.svg) | |
-K252a_1R0P.png) | |
| Names | |
|---|---|
| Preferred 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-carboxylate | |
| Identifiers | |
| ChEMBL | |
| ChemSpider |
|
| ECHA InfoCard | 100.167.781 |
| UNII | |
| |
| Properties[1] | |
| C27H21N3O5 | |
| Molar mass | 467.481 g·mol−1 |
| Solubility in other solvents | Soluble inDMSO,dichloromethane, andmethanol |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
K252a is analkaloid isolated fromNocardiopsisbacteria. Thisstaurosporine analog is a highly potent cell permeableinhibitor of CaMkinase and phosphorylase kinase (IC50 = 1.8 and 1.7nmol/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 forpsoriasis.[11]
K252a inhibits tyrosinephosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10ng/ml NGF with or without various concentrations of K252a.
