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IU1

Cat. No. M2035
IU1 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 65  USD65 In stock
10mg USD 88  USD88 In stock
25mg USD 185  USD185 In stock
50mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

IU1 is an inhibitor of USP14, a deubiquitinating enzyme associated with the proteasome. The proteasome mediates the cellular degradation of oxidized, damaged and misfolded proteins which, if not removed, accumulate and become toxic to cells. USP14 is one of several deubiquitinating enzymes (DUBs) responsible for shortening proteasome-bound ubiquitin chains, which is known to antagonize the degradation of ubiquitin-protein conjugates. IU1 inhibits the catalytic activity of proteasome-associated Usp14 in vitro (IC50 < 4 μM). IU1 selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress. IU1 may help to eliminate toxic proteins more effectively by enhancing their degradation.

Product Citations
Customer Product Validations & Biological Datas
Source Am J Physiol Renal Physiol (2016). Figure 2. IU1
Method immunoblots
Cell Lines GEC
Concentrations 50 μM
Incubation Time 24 h
Results After 4 or 6 h of treatment with IUI, the levels of GFPu were reduced compared with untreated, implying that inhibition of wild-type Usp14 resulted in enhanced UPS activity
Chemical Information
Molecular Weight 300.37
Formula C18H21FN2O
CAS Number 314245-33-5
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lee BH, et al. Nature. Enhancement of proteasome activity by a small-molecule inhibitor of USP14.

[2] Lee MJ, et al. Mol Cell Proteomics. Trimming of ubiquitin chains by proteasome-associated deubiquitinating enzymes.

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Keywords: IU1 supplier, Proteasome, inhibitors, activators


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