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K252b is a cell membrane-impermeable analog of staurosporine that inhibits PKC. K252b inhibits production of hepatocyte growth factor and inhibits synthesis of DNA in vitro. K252b also inhibits various microbial ectoprotein kinases (those which are expressed on membrane surfaces). Additionally, K252b inhibits IgE cross-linking-dependent degranulation in basophils.
| Cas No. | 99570-78-2 |
|---|---|
| Purity | ≥98% |
| Formula | C26H16N3O5 |
| Formula Wt. | 453.13 |
| IUPAC Name | (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylic acid |
| Synonym | Protein Kinase Inhibitor K-252B |
| Solubility | DMSO or Methanol |
| Appearance | Off White Powder |
| Store Temp | 4°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Lecht S, Arien-Zakay H, Kohan M, et al. Angiostatic effects of K252a, a Trk inhibitor, in murine brain capillary endothelial cells. Mol Cell Biochem. 2010 Jun;339(1-2):201-13. PMID: 20148355.
Okada M, Hojo Y, Ikeda U, et al. Interaction between monocytes and vascular smooth muscle cells induces expression of hepatocyte growth factor. J Hypertens. 2000 Dec;18(12):1825-31. PMID: 11132607.
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. 1997 Jul 15;159(2):964-9. PMID: 9218617.
Hogan MV, Pawlowska Z, Yang HA, et al. Surface phosphorylation by ecto-protein kinase C in brain neurons: a target for Alzheimer's beta-amyloid peptides. J Neurochem. 1995 Nov;65(5):2022-30. PMID: 7595486.
Lagoo A, Tseng CK, Sell S. Molecular signals in B cell activation. II. IL-2-mediated signals are required in late G1 for transition to S phase after ionomycin and PMA treatment. Cell Immunol. 1990 May;127(2):497-505. PMID: 2328536.