生物活性 | |||
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描述 | Protein tyrosine phosphatases (PTPs) play a multifunctional role in coordinating signaling networks. BVT 948 is an inhibitor of PTPs with IC50 values of 0.9±0.3μM, 1.7±0.1μM, 0.09±0.01μM, 1.5±0.4μM, and 0.7±0.05μM for PTP1B, TCPTP, SHP-2, LAR, and YopH, respectively. It also exhibited robust inhibitory effects against several cytochrome P450 isoforms in vitro. BVT 948 at a concentration of 25μM stimulated glucose uptake into L6 myotubes in a PI3K-dependent fashion. Mice treated with 3μmol/kg BVT 948 showed significantly increased glucose clearance from the bloodstream in response to insulin compared with the vehicle-treated group.[1] | ||
作用机制 | BVT 948 is a noncompetitive inhibitor of PTP. It irreversibly inhibits PTP1B activity in vitro by catalyzing the catalytic cysteine residue of the enzyme.[1] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.15mL 0.83mL 0.41mL |
20.73mL 4.15mL 2.07mL |
41.45mL 8.29mL 4.15mL |
参考文献 |
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