生物活性 | |||
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描述 | PTP1B-IN-2 exhibits selectivity for PTP1B that is over 40 times greater than for SHP-2 and LAR, and it is 15 times more selective for PTP1B compared to TCPTP, which is closely related. The compound PTP1B-IN-2 penetrates the active site pocket deeply, establishing multiple hydrogen bonds and hydrophobic contacts with essential residues at the catalytic site. The interaction profile of PTP1B-IN-2 with the PTP1B domain indicates it is an ABC type inhibitor, affecting not just the catalytic site but also the B and C sites. PTP1B-IN-2 significantly boosts insulin-induced IRβ phosphorylation at 15 μM and 30 μM concentrations. Moreover, it notably augments insulin-driven glucose absorption in L6 myotubes, with increases of 16.0%, 19.0%, and 38.1% observed at concentrations of 5, 10, and 20 μM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.47mL 0.29mL 0.15mL |
7.34mL 1.47mL 0.73mL |
14.69mL 2.94mL 1.47mL |