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Biological Data
| Biological description | Non-selective protein kinase inhibitor (IC50 values are 10-30 nM for serine/threonine protein kinases). PKC and Ca2+ / calmodulin-stimulated phosphodiesterase inhibitor (IC50 values are 32.9 nM and 1.8 - 2.8 µM respectively). Competitively inhibits myosin light chain kinase (MLCK) - may interact with the ATP-binding domain (Ki = 20 nM). Blocks neuronal differentiation by potently inhibiting NGF receptor gp140trk tyrosine protein kinase (IC50 = 3nM). Cell permeable and shows potential anti-tumor actions. |
Solubility & Handling
| Storage instructions | -20°C |
| Solubility overview | Soluble in DMSO (1mg/ml) or DMF (1mg/ml) |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical 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 methyl ester |
| Chemical structure | ![K-252a [99533-80-9] Chemical Structure](data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAAAEAAAABCAQAAAC1HAwCAAAAC0lEQVR4nGP6zwAAAgcBApocMXEAAAAASUVORK5CYII= "K-252a [99533-80-9]") |
| Molecular Formula | C27H21N3O5 |
| PubChem identifier | 3035817 |
| SMILES | C[C@@]12[C@](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(C(=O)OC)O |
| InChi | 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 |
| InChiKey | KOZFSFOOLUUIGY-SOLYNIJKSA-N |
References for K-252a
References are publications that support the biological activity of the product
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K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors.
Tapley P et al (1992) Oncogene 7(2) : 371-81. -
K-252a, a novel microbial product, inhibits smooth muscle myosin light chain kinase.
Nakanishi S et al (1988) J Biol Chem 263(13) : 6215-9. -
The effect of K-252a, a potent microbial inhibitor of protein kinase, on activated cyclic nucleotide phosphodiesterase.
Matsuda Y et al (1988) Biochem J 256(1) : 75-80. -
K-252a, a potent inhibitor of protein kinase C from microbial origin.
Kase H et al (1986) J Antibiot (Tokyo) 39(8) : 1059-65.
Non-selective protein kinase inhibitor
![K-252a [99533-80-9] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb0351.png "K-252a [99533-80-9]")
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