| Identification | Back Directory | [Name]
K-252B | [CAS]
99570-78-2 | [Synonyms]
K-252B
KT 5556
k-252b solution
K252B READY MADE
Antibiotic K 252b
K-252B, NOCARDIOPSIS SP
K-252B, NOCARDIOPSIS SPECIES
PROTEIN KINASE INHIBITOR K-252B
K252b Antibiotic K 252b KT 5556
(9R,10S,12S)-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
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, (9S,10R,12R)- | [EINECS(EC#)]
999-999-2 | [Molecular Formula]
C26H19N3O5 | [MDL Number]
MFCD00132117 | [MOL File]
99570-78-2.mol | [Molecular Weight]
453.45 |
| Chemical Properties | Back Directory | [Boiling point ]
769.8±60.0 °C(Predicted) | [density ]
1.78±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
Soluble in DMSO (up to 1 mg/ml) or in DMF (up to 1 mg/ml). | [form ]
ready-to-use solution
| [pka]
3.33±0.40(Predicted) | [color ]
White or off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C.1 However, as this compound does not freely pass through the cell membrane, it is used to inhibit extracellular kinases (ectokinases) of cells in culture.2,3 K252b inhibits receptor-mediated degranulation from basophil-like RBL-2H3 cells (IC50 = 0.5 μg/ml) and human basophils.4 This extracellular inhibitor is also used in comparison studies with the closely related, cell-permeable inhibitor K252a, particularly in studies of neuronal differentiation.5,6 | [Chemical Properties]
Yellow solid | [Uses]
K252A is a staurosporine analogue isolated from a Nocardiopsis strain as a potent inhibitor of protein kinase C. K252A exhibits potent antitumour activity but shows no antimicrobial activity in vitro, or in vivo toxicity in rodents. While K252A is a potent inhibitor of Ca2+/calmodulin kinase II, it is also active against other kinases, notably myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and cGMP-dependent protein kinase (PKG). | [storage]
Store at -20°C | [References]
1) Kase et al. (1987), K252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436
2) Makino et al. (2012), Inhibition of uterine sarcoma cell growth through suppression of endogenous tyrosine kinase B signaling; PLoS One, 7 e41049 |
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Lynnchem
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Novachemistry
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