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Submit ReviewDamnacanthal is a potent inhibitor of p56lck tyrosine kinase activity (IC50 = 17 nM for inhibition of autophosphorylation). Displays 7- to 20-fold selectivity over p59fyn and p60src tyrosine kinases, > 40-fold selectivity over c-ErbB2, EGF- and insulin-receptor tyrosine kinases, and > 100-fold selectivity over PKA and PKC. Mobilizes intracellular Ca2+ in dermal fibroblasts and inhibits Ras function. Also inhibits LIMK1/2, as well as migration and invasion of breast cancer cells in vitro.
分子量 | 282.25 |
公式 | C16H10O5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 477-84-9 |
PubChem ID | 2948 |
InChI Key | IPDMWUNUULAXLU-UHFFFAOYSA-N |
Smiles | O=C2C3=C(C=C(O)C(C=O)=C3OC)C(C1=CC=CC=C12)=O |
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.
参考文献是支持产品生物活性的出版物。
Hiramatsu et al (1993) Induction of normal phenotypes in ras-transformed cells by damnacanthal from Morinda citrifolia. Cancer Lett. 73 161 PMID: 7693328
Faltynek et al (1995) Damnacanthal is a highly potent, selective inhibitor fo p56lck tyrosine kinase activity. Biochemistry 34 12404 PMID: 7547985
Aoki et al (2000) Mechanism of damnacanthal-induced [Ca2+]i elevation in human dermal fibroblasts. Eur.J.Pharmacol. 387 119 PMID: 10650151
关键词: Damnacanthal, Damnacanthal supplier, potent, inhibitors, inhibits, p56lck, kinases, selective, Src, Kinases, LIMK, 1936, Tocris Bioscience
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