A non-selective PKC inhibitor
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K252a

Item No. 11338

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3,9S,10R,11,12R-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, methyl ester
CAS Number
99533-80-9
Synonyms
  • SF 2370
Molecular Formula
C27H21N3O5
Formula Weight
467.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Dichloromethane: 5 mg/mlDMSO: 50 mg/mlMethanol: 2 mg/ml
λmax
290 nm
SMILES
O[C@@]1(C(OC)=O)[C@@](O[C@]2([H])C1)(C)N3C4=CC=CC=C4C5=C3C(N2C6=CC=CC=C67)=C7C8=C5CNC8=O
InChi Code
InChI=1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)/t18-,26+,27+/m1/s1
InChi Key
KOZFSFOOLUUIGY-SOLYNIJKSA-N
Origin
Bacterium/Nocardiopsis sp.
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    K252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi that inhibits protein kinase (PK) C, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase with IC50 values of 470, 140, 270, and 1.7 nM, respectively.1,2 Because it inhibits neurotrophin receptor tyrosine kinases, K252a at 100-500 nM has been used to suppress trophoblast proliferation and increase apoptosis associated with the disruption of mitochondrial functions in cultured choriocarcinoma cells.3 Recently, K252a has been shown to inhibit PRK1 (IC50 = 3.2 nM in vitro), a PKC-related kinase that phosphorylates histone H3 at threonine 11 and is involved in androgen-dependent gene expression.4

    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. Davis, P.D., Hill, C.H., Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. J. Med. Chem. 35(1), 177-184 (1992).

    3. 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).

    4. Köhler, J., Erlenkamp, G., Eberlin, A., et al. Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells. PLoS One 7(4), (2012).