产品说明
一般描述
A cell-permeable flavanoid that displays anti-inflammatory, anti-diabetic and anti-cancer properties. Acts as a non-ATP competitive MEK1 inhibitor (IC50<3 µM), and ATP-competitive inhibitors of CKI, CKII, IR, MLCK, PKA and PKC (Ki = 9.0 µM, 0.6 µM, 2.6 µM, 1.7 µM, 27.5 µM and 12.1 µM, respectively) and PI 3-Kα and PIM-1 (IC50 = 1.8 µM and 0.78 µM). Reported to inhibit the activities of phosphodiesterase 1-4 (IC50<40 µM) and MMP-2 (IC50<24 µM in several colorectal carcinoma cells), and block TNFα-mediated NF-κB signaling (at 50 µM in ECV304 cells) and insulin-stimulated glucose transport (Ki ~ 33.5 µM in rat adipocytes). Further, induce apoptosis in HL-60 leukemia cells with an IC50 of 43 µM.
A cell-permeable flavanoid that displays anti-inflammatory, anti-diabetic and anti-cancer properties. Acts as a non-ATP competitive MEK1 inhibitor (IC50<3 µM), and ATP-competitive inhibitors of CKI, CKII, IR, MLCK, PKA and PKC (Ki = 9.0 µM, 0.6 µM, 2.6 µM, 1.7 µM, 27.5 µM and 12.1 µM, respectively) and PI 3-Kα and PIM-1 (IC50 = 1.8 µM and 0.78 µM). Reported to inhibit the activities of phosphodiesterase 1-4 (IC50<40 µM) and MMP-2 (IC50<24 µM in several colorectal carcinoma cells), and block TNFα-mediated NF-κB signaling (at 50 µM in ECV304 cells) and insulin-stimulated glucose transport (Ki = ~ 33.5 µM in rat adipocytes). Further, induce apoptosis in HL-60 leukemia cells with an IC50 of 43 µM.
包装
25 mg in Plastic ampoule
Packaged under inert gas
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
Lee, K.W., et al. 2007. Carcinogenesis28, 1918.
Holder, S., et al. 2007. Mol. Cancer Ther.6, 163.
Strobel, P., et al. 2005. Biochem. J.386, 471.
Ko, C.H., et al. 2005. Mol. Cancer Ther.4, 281.
Ko, C.H., et al. 2005. Biochem. Pharmacol.69, 913.
Ko, W.C., et al. 2004. Biochem. Pharmacol.68, 2087.
Walker, E.H., et al. 2000. Mol. Cell6, 909.
Agullo, G., et al. 1997. Biochem. Pharmacol.53, 1649.
Hagiwara, M., et al. 1988. Biochem. Pharmacol.37, 2987.
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 | C15H10O8 |
分子量 | 318.24 |
MDL编号 | MFCD00006827 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | yellow-brown |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
InChI | 1S/C15H10O8/c16-6-3-7(17)11-10(4-6)23-15(14(22)13(11)21)5-1-8(18)12(20)9(19)2-5/h1-4,16-20,22H |
InChI key | IKMDFBPHZNJCSN-UHFFFAOYSA-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