For research use only. Not for therapeutic Use.
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].
Catalog Number | I019023 |
CAS Number | 670270-31-2 |
Synonyms | 1-[1-(4-chlorophenyl)-2,5-dimethylpyrrol-3-yl]-2-piperidin-1-ylethanone |
Molecular Formula | C19H23ClN2O |
Purity | ≥95% |
InChI | InChI=1S/C19H23ClN2O/c1-14-12-18(19(23)13-21-10-4-3-5-11-21)15(2)22(14)17-8-6-16(20)7-9-17/h6-9,12H,3-5,10-11,13H2,1-2H3 |
InChIKey | VXQIPRWKLACSKZ-UHFFFAOYSA-N |
SMILES | CC1=CC(=C(N1C2=CC=C(C=C2)Cl)C)C(=O)CN3CCCCC3 |
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. |