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.
IC50&Target
IC50: 0.6 μM (USP14), 20 μM (IsoT/USP5)
体外研究
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.
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.
Western Blot Analysis
Cell Line:
Murine cortical primary neurons (DIV5) isolated from APPSwe/P301L transgenic animals
Concentration:
3 μM, 10 and 30 μM
Incubation Time:
48 hours
Result:
Significantly decreased Tau and phosphotau species Ser-202/Thr-205 levels. No change in USP14 protein level.
分子式
C19H23ClN2O
分子量
330.85
CAS号
670270-31-2
运输条件
Room temperature in continental US; may vary elsewhere.