产品说明
一般描述
A macrocyclic lactone that exhibits anti-tumor properties. Potently activates protein kinase C and exhibits high binding affinity (Ki = 1.35 nM). Effectively translocates protein kinase C (PKC) isozymes α, β, and ε and induces a biphasic, concentration-dependent, down-regulation of PKC δ. Reported to compete with phorbol esters in binding to PKC. Stimulates protein kinase D (PKD) activity in a biphasic, PKC-dependent manner in intact cells. Also activates Ras in Jurkat T cells and in rat2 cells.
A macrocyclic lactone with antitumor properties. Potently activates protein kinase C and exhibits a high binding affinity (Ki = 1.35 nM). Effectively translocates and down-regulates PKC isozymes α, δ, and ε. Induces a biphasic activation of PKD through a PKC-dependent pathway in intact cells. Also shown to activate Ras in Jurkat T cells and in rat2 cells.
包装
10 μg in Plastic ampoule
生化/生理作用
Target Ki: 1.35 nM for protein kinase C
Product does not compete with ATP.
Reversible: no
Primary Target
Protein kinase C
Cell permeable: no
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Clamp, A., and Jayson, G. 2002. Anticancer Drugs13, 673.
Lorenzo, P.S., et al. 1999. Cancer Res.59, 6137.
Wang, Q.J., et al. 1999. J. Biol. Chem.274, 37233.
Wender, P.A., et al. 1998. Proc. Natl. Acad. Sci. USA95, 6624.
Matthews, S.A., et al. 1997. J. Biol. Chem.272, 20245.
Szallasi, Z., et al. 1994. Mol. Pharmacol.46, 840.
Berkow, R.L., and Kratt, A.S. 1985. Biochem. Biophys. Res. Commun.3, 1109.
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 | C47H68O17 |
分子量 | 905.03 |
MDL编号 | MFCD00893832 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | film solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | white to colorless |
溶解性 | DMSO: 25 mg/mL ethanol: 25 mg/mL |
运输 | ambient |
储存温度 | −20℃ |
InChI | 1S/C47H68O17/c1-10-11-12-13-14-15-39(51)62-43-31(22-41(53)58-9)21-34-25-37(28(2)48)61-42(54)24-32(50)23-35-26-38(59-29(3)49)45(6,7)46(55,63-35)27-36-19-30(20-40(52)57-8)18-33(60-36)16-17-44(4,5)47(43,56)64-34/h12-17,20,22,28,32-38,43,48,50,55-56H,10-11,18-19,21,23-27H2,1-9H3/b13-12+,15-14+,17-16+,30-20+,31-22+/t28-,32-,33+,34+,35?,36?,37?,38?,43+,46+,47-/m1/s1 |
InChI key | MJQUEDHRCUIRLF-BXOMOELISA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich