产品说明
一般描述
A cell-permeable, potent, reversible, and selective inhibitor of p56lck tyrosine kinase activity. Inhibits p56lck autophosphorylation (IC50 = 17 nM) and phosphorylation of an exogenous peptide by p56lck over PKA and PKC and >40 fold selectivity for p56lck over EGF, c-erbB2, insulin, and the PDGF receptor tyrosine kinases. In addition, damnacanthal exhibits 7-20 fold selectivity for p56lck over pp60src and pp59fyn. Inhibition of p56lck by damnacanthal appears to be reversible, not time-dependent and not significantly affected by the presence of sulfhydryl reagents. Also known to have antimalarial properties, and to reverse the phenotype of ras-transformed cells.
A cell-permeable, potent, reversible, and selective inhibitor of p56lck tyrosine kinase. Inhibits p56lck autophosphorylation (IC50 = 17 nM) and phosphorylation of an exogenous peptide by p56lck (IC50 = 620 nM). Exhibits over 100-fold greater selectivity for p56lck over PKA and PKC, 40-fold greater selectivity for p56lck over EGF receptor kinase, c-ErbB2, insulin receptor kinase, and PDGF receptor kinase, and 7 - 20-fold greater selectivity for p56lck over p60src and p59fyn. Inhibition of p56lck is not significantly affected by the presence of sulfhydryl reagents. Also known to have antimalarial properties and to reverse the phenotype of ras-transformed cells.
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
p56lck autophosphorylation
Target IC50: 17 nM against p56lck autophosphorylation
Product does not compete with ATP.
Reversible: yes
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他说明
Faltynek, C.R., et al. 1995. Biochemistry34, 12404.
Hiramatsu, T., et al. 1993. Cancer Lett.73, 161.
Koumaglo, K., et al. 1992. Planta Med.58, 533.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C16H10O5 |
分子量 | 282.25 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | orange-yellow |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | −20℃ |
InChI | 1S/C16H10O5/c1-21-16-11(7-17)12(18)6-10-13(16)15(20)9-5-3-2-4-8(9)14(10)19/h2-7,18H,1H3 |
InChI key | IPDMWUNUULAXLU-UHFFFAOYSA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |