IU1

Names

[ Name ]:
IU1

[Synonym ]:
Ethanone, 1-[1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)-
IU1
F1142-1244
1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone
Usp14 inhibitor

Biological Activity

[Description]:

IU1 is a special Usp14 inhibitor with IC50 of 4-5 μM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Deubiquitinase

Research Areas >> Cardiovascular Disease

[Target]

IC50: 4-5 μM (Usp14)[1]

[In Vitro]

Usp14, a proteasome-associated deubiquitinating enzyme, can inhibit the degradation of ubiquitin-protein conjugates, in vivo and in vitro. IU1inhibits the catalytic activity of proteasome associated Usp14 in vitro. The IC50 of IU1 for Usp14 is 4-5 μM. IU1 binds specifically to the activated form of Usp14. IU1 can potentially inhibit Usp14 by preventing its docking on the proteasome, but direct tests of this scenario proved negative. Usp14 inhibition is rapidly established upon addition of IU1 and rapidly reversed upon its removal. IU1 also promotes degradation of Sic1, a CDK inhibitor from S. cerevisiae[1].

[References]

[1]. Lee BH, et al. Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature. 2010 Sep 9;467(7312):179-84.

[Related Small Molecules]

BAY 11-7082 | P5091 | PR-619 | VLX1570 | Degrasyn(WP1130) | P 22077 | DUBs-IN-2 | ML364 | NSC 687852 | GNE-6776 | ML 323 | HBX 19818 | LDN-57444 | USP7/USP47 inhibitor

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
437.0±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₁FN₂O

[ Molecular Weight ]:
300.371

[ Flash Point ]:
218.1±28.7 °C

[ Exact Mass ]:
300.163788

[ PSA ]:
25.24000

[ LogP ]:
4.07

[ Appearance of Characters ]:
off-white to light brown

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.585

[ Storage condition ]:
Store at +4°C

[ Water Solubility ]:
DMSO: >10mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS05

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H318

[ Precautionary Statements ]:
P280-P305 + P351 + P338

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
41

[ Safety Phrases ]:
61

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Post-endocytotic Deubiquitination and Degradation of the Metabotropic γ-Aminobutyric Acid Receptor by the Ubiquitin-specific Protease 14.

J. Biol. Chem. 291 , 7156-70, (2016)

Mechanisms controlling the metabotropic γ-aminobutyric acid receptor (GABAB) cell surface stability are still poorly understood. In contrast with many other G protein-coupled receptors (GPCR), it is n...

Ubiquitin-specific protease 14 modulates degradation of cellular prion protein.

Sci. Rep. 5 , 11028, (2015)

Prion diseases are fatal neurodegenerative disorders characterized by the accumulation of prion protein (PrP(C)). To date, there is no effective treatment for the disease. The accumulated PrP, termed ...

IU1