K252b

Names

[ Name ]:
K252b

[Synonym ]:
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylicacid,2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-,(9S,10R,12R)
K-252b solution
MFCD00132117
(15R,16S,18S)-16-Hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1.0.0.0.0.0]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylic acid
6,9-Epoxy-15H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-7-carboxylic acid, 6,7,8,9,16,17-hexahydro-7-hydroxy-6-methyl-15-oxo-, (6R,7S,9S)-
(5R,6S,8S)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13H-5,8-epoxy-4b,8a,14-triazadibenzo[b,h]cycloocta[1,2,3,4-jkl]cyclopenta[e]-as-indacene-6-carboxylic acid

Biological Activity

[Description]:

K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely [1][2][3].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Infection

Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

PKC[1].

[References]

[1]. Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39(8), 1072-1078 (1986).

[2]. Plomp, J.J., et al. Involvement of protein kinases in the upregulation of acetylcholine release at endplates of α-bungarotoxin-treated rats Journal of Physiology 493, 175-186 (1996).

[3]. Zhu, X., et al. Evidence of ectokinase-mediated phosphorylation of osteopontin and bone sialoprotein by osteoblasts during bone formation in vitro Biochemistry Journal 323, 637-643 (1997).

Chemical & Physical Properties

[ Density]:
1.8±0.1 g/cm3

[ Boiling Point ]:
769.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₁₉N₃O₅

[ Molecular Weight ]:
453.446

[ Flash Point ]:
419.4±32.9 °C

[ Exact Mass ]:
453.132477

[ PSA ]:
105.72000

[ LogP ]:
3.57

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.903

Safety Information

[ Hazard Codes ]:
Xi: Irritant;

[ RIDADR ]:
UN 1993 / PGIII

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Cooperativity between extracellular adenosine 5'-triphosphate and activation of N-methyl-D-aspartate receptors in long-term potentiation induction in hippocampal CA1 neurons.

Neuroscience 113 , 617-628, (2002)

The mechanism of ATP-induced long-term potentiation (LTP) was studied pharmacologically using guinea-pig hippocampal slices. LTP, induced in CA1 neurons by 10 min application of 10 microM ATP, was blo...