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Submit ReviewK 252a is a non-selective protein kinase inhibitor; analog of staurosporine (Cat.No. 1285). Inhibits PKC (IC50 = 32.9 nM), Ca2+/calmodulin-stimulated phosphodiesterases (IC50 = 1.3 - 2.9 μM), MLCK (Ki = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).
分子量 | 467.48 |
公式 | C27H21N3O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 99533-80-9 |
PubChem ID | 3035817 |
InChI Key | KOZFSFOOLUUIGY-SOLYNIJKSA-N |
Smiles | [H][C@](C[C@]8(O)[C@@](OC)=O)(O[C@]78C)N5C3=C2N7C1=CC=CC=C1C2=C(CNC6=O)C6=C3C4=CC=CC=C45 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 11.69 | 25 |
以下数据基于产品分子量 467.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.25 mM | 8.56 mL | 42.78 mL | 85.57 mL |
1.25 mM | 1.71 mL | 8.56 mL | 17.11 mL |
2.5 mM | 0.86 mL | 4.28 mL | 8.56 mL |
12.5 mM | 0.17 mL | 0.86 mL | 1.71 mL |
参考文献是支持产品生物活性的出版物。
Kase et al (1986) K-252a, a potent inhibitor of protein kinase C from microbial origin. J.Antibiot. 39 1059 PMID: 3759657
Knusel and Hefti (1992) K-252 compounds: modulators of neurotrophin signal transduction. J.Neurochem. 59 1987 PMID: 1431889
Morotti et al (2002) K252a inhibits the oncogenic properties of Met, the HGF receptor. Oncogene 21 4885 PMID: 12118367
Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. TiPS 10 218 PMID: 2672462
If you know of a relevant reference for K 252a, please let us know.
关键词: K 252a, K 252a supplier, Protein, kinase, inhibitor, kinases, inhibitors, receptor, tyrosine, inhibits, cMET, HGF, K252a, SF2370, SF, 2370, Broad, Spectrum, Kinase, Inhibitors, MET, Receptors, 1683, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 K 252a 的部分引用包括:
Martín-Segura et al (2019) Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism. Front Neurol 10 675 PMID: 31293510
Chen et al (2014) BDNF released during neuropathic pain potentiates NMDA receptors in primary afferent terminals. Eur J Neurosci 39 1439 PMID: 24611998
Pandya and Pillai (2014) TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis. Biomed Res Int 12 47 PMID: 25052836
Schubert et al (2014) Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis. Acta Neuropathol 128 835 PMID: 25341622
Park et al (2013) Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging. Mol Cells 38 1426 PMID: 23389690
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Kummer and Cohen (2015) Exercise-induced neuroprotection in the spastic Han Wistar rat: the possible role of brain-derived neurotrophic factor. Neuropsychopharmacology 2015 834543 PMID: 25710032
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