A cell-impermeable kinase inhibitor
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K252b

Item No. 11339

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
99570-78-2
Molecular Formula
C26H19N3O5
Formula Weight
453.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Methanol: 2 mg/ml
λmax
231, 250, 291, 336, 351 368 nm
SMILES
O[C@]1(C(O)=O)[C@](O[C@@]2([H])C1)(C)N3C4=CC=CC=C4C5=C3C(N2C6=CC=CC=C67)=C7C8=C5CNC8=O
InChi Code
InChI=1S/C26H19N3O5/c1-25-26(33,24(31)32)10-17(34-25)28-15-8-4-2-6-12(15)19-20-14(11-27-23(20)30)18-13-7-3-5-9-16(13)29(25)22(18)21(19)28/h2-9,17,33H,10-11H2,1H3,(H,27,30)(H,31,32)/t17-,25+,26+/m1/s1
InChi Key
AMSOPBXQXSAAAC-PLZPTFKGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $215

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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yasuzawa, T., Iida, T., Yoshida, M., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c and d. J. Antibiot. (Tokyo) 39(8), 1072-1078 (1986).

    2. Plomp, J.J., and Molenaar, P.C. Involvement of protein kinases in the upregulation of acetylcholine release at endplates of α-bungarotoxin-treated rats. J. Physiol. 493(Pt 1), 175-186 (1996).

    3. Zhu, X., Luo, C., Ferrier, J.M., et al. Evidence of ectokinase-mediated phosphorylation of osteopontin and bone sialoprotein by osteoblasts during bone formation in vitro. Biochem. J. 323(Pt 3), 637-643 (1997).

    4. Teshima, R., Saito, Y., Ikebuchi, H., et al. Effect of an ectokinase inhibitor, K252b, on degranulation and Ca2+ signals of RBL-2H3 cells and human basophils. J. Immunol. 159(2), 964-969 (1997).

    5. Thompson, A.F., and Levin, L.A. Neuronal differentiation by analogs of staurosporine. Neurochem. Int. 56(4), 554-560 (2010).

    6. Kawamura, N., Kawamura, K., Manabe, M., et al. Inhibition of brain-derived neurotrophic factor/tyrosine kinase B signaling suppresses choriocarcinoma cell growth. Endocrinology 151(7), 3006-3014 (2010).