1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. IU1-47

IU1-47 

Cat. No.: HY-122243 Purity: 99.76%
Handling Instructions

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.

For research use only. We do not sell to patients.

IU1-47 Chemical Structure

IU1-47 Chemical Structure

CAS No. : 670270-31-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 290 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

IC50: 0.6 μM (USP14), 20 μM (IsoT/USP5)[1]

In Vitro

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: 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.
Molecular Weight

330.85

Formula

C₁₉H₂₃ClN₂O

CAS No.

670270-31-2

SMILES

CC1=CC(C(CN2CCCCC2)=O)=C(N1C3=CC=C(C=C3)Cl)C

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (50.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0225 mL 15.1126 mL 30.2252 mL
5 mM 0.6045 mL 3.0225 mL 6.0450 mL
10 mM 0.3023 mL 1.5113 mL 3.0225 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (5.05 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (5.05 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (5.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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IU1-47
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HY-122243
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