BVT 948 is a non-competitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTPs) with IC50 of 0.09 - 1.7 μM, displaying irreversible inhibition through catalysis of the hydrogen peroxide-dependent oxidation of PTP. BVT 948 enhances insulin signaling in vitro and insulin tolerance in ob/ob mice in vivo.
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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] |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 39674-97-0 |
分子式 | C14H11NO3 |
分子量 | 241.242 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(435.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |