IU1-47 是一种有效的特异性 USP14 抑制剂，IC50 为 0.6 μM。IU1-47 抑制 IsoT/USP5， IC50 为 20 μM。IU1-47 在培养的神经元中诱导 tau 蛋白降解。
货号:ajcx38630
CAS:670270-31-2
分子式:C19H23ClN2O
分子量：330.85
溶解度:DMSO : 16.67 mg/mL (50.39 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons[1].

IU1-47 is essentially inactive on free USP14 (USP14 that is not bound to the proteasome). IU1-47 (25 μM) antagonizes USP14 deubiquitinating activity and stimulates substrate degradation in vitro[1]. IU1-47 stimulates tau degradation principally via the ubiquitin-proteasome system. IU1-47 (3 μM, 10 and 30 μM; 48 hours) significantly decreases Tau and phosphotau species Ser-202/Thr-205 levels in murine cortical primary neurons. The level of USP14 itself does not change[1].

[1]. Boselli M, et al. An inhibitor of the proteasomal deubiquitinating enzyme USP14 induces tau elimination in cultured neurons. J Biol Chem. 2017 Nov 24;292(47):19209-19225.