General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow-brown |
| solubility | DMSO: 5 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [o]1c2c([c](c(c1c3cc(c(c(c3)O)O)O)O)=O)c(cc(c2)O)O |
| 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 |
