Names | |
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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 |
PubChem
CID
|
|
UNII | |
CompTox Dashboard (
EPA)
|
|
| |
Properties [1] | |
C27H21N3O5 | |
Molar mass | 467.481 g·mol−1 |
Solubility in other solvents | Soluble in DMSO, dichloromethane, and methanol |
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
|
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 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.
The Scientific World Journal; Volume 2013, Article ID 980419; https://dx.doi.org/10.1155/2013/980419
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 |
PubChem
CID
|
|
UNII | |
CompTox Dashboard (
EPA)
|
|
| |
Properties [1] | |
C27H21N3O5 | |
Molar mass | 467.481 g·mol−1 |
Solubility in other solvents | Soluble in DMSO, dichloromethane, and methanol |
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
|
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 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.
The Scientific World Journal; Volume 2013, Article ID 980419; https://dx.doi.org/10.1155/2013/980419