| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 20mg | 电议 |
Preparation Method | For studies of the kinetics of inhibition of PtdIns-3-kinase by wortmannin, bovine brain enzyme was incubated with 0 to 14 nM wortmannin with varying ATP concentrations from 2.5 to 20 μM. For studies of the time course of PtdIns-3-kinase inhibition, wortmannin 0 to 14 nM, enzyme, and PtdIns were incubated for various times at room temperature before adding [γ-32P]ATP to start the reaction. |
Reaction Conditions | 0-14 nM wortmannin |
Applications | Kinetic analysis demonstrates that wortmannin is a noncompetitive, irreversible inhibitor of phosphatidylinositol-3-kinase, with inactivation being both time- and concentration-dependent. |
Cell lines | Jurkat cells |
Preparation Method | Jurkat-soluble fractions were treated with AX7503 (50 nM) for 60 min with or without preincubation with various concentrations of wortmannin (0.25?0 nM) or LY294002 (10?0,000 nM) for 10 min. |
Reaction Conditions | Wortmannin (0.25?0 nM) for 10 min |
Applications | PLK1 activity was inhibited by wortmannin with an IC 50 value of 24 nM. |
Animal models | Scid mice |
Preparation Method | Oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period. |
Dosage form | 1 mg/kg for 14 days; 1.5 mg/kg for 5 days + 1.0 mg/kg for 9 days. |
Applications | Wortmannin treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation. |
| 文献引用 | |
| 产品描述 | Wortmannin is a highly potent direct inhibitor of PI3-kinase specificity originally derived from fungi (1,2). This inhibition is irreversible and non-competitive with an IC50 of 3 nM[2][3]. Wortmannin does not inhibit PI4 kinase, protein kinase C, or protein tyrosine kinases[4]. In Jurkat cell, at the concentrations of wortmannin commonly used to inhibit PI 3-kinases, PLK1 is also significantly inhibited[5]. In Swiss 3T3 cells, Wortmannin is a selective and reversible phosphatidylinositol 3-kinase inhibitor with an IC50 value of 1.9 nM[4].PI3-kinase is involved in the signal transduction pathway responsible for histamine secretion following stimulation of Fc epsilon RI and that wortmannin blocks these responses through direct interaction with the catalytic subunit of this enzyme[1]. Wortmannin treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[6]. Wortmannin inhibits myosin light chain phosphorylation and contraction in rat aorta. As an inhibitor of MLCK, wortmannin can be used as a vasodilator and anti-inflammatory agent[7]. References: |
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