| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.6 μM (USP14), 20 μM (IsoT/USP5) | ||||||||||||
| Invitro | 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]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | IU1-47 | ||||||||||||
| CAS | 670270-31-2 | ||||||||||||
| Formula | C19H23ClN2O | ||||||||||||
| Molar Mass | 330.85 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |