商品编号


2978/10



品牌


Tocris



公司


Bio-Techne Corporation



公司分类


Ligases



Size

10 mg

商品信息

Description:
Ubiquitin-activating enzyme (E1) inhibitor

Chemical Name:
4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester

Purity:
≥98% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Cell-permeable, irrevers
IBL
e ubiquitin-activating enzyme (E1) inhibitor (IC
50
< 10
μ
M). Blocks ubiquitination and prevents ubiquitin-mediated proteasomal degradation. Inhibits NF-
κ
B activation, blocks degradation of p53, increases p21 levels and induces apoptosis
in vitro
. Also causes an increase in sumoylation of proteins.



Technical Data



M. Wt

371.3



Formula

C
17
H
13
N
3
O
7




Storage

Store at -20°C



Purity

≥98% (HPLC)



CAS Number

418805-02-4



PubChem ID

2856906



InChI Key

ARGIPZKQJGFSGQ-UHFFFAOYSA-N



Smiles

CCOC(=O)C1=CC=C(C=C1)N1NC(=O)C(=CC2=CC=C(O2)[N+]([O-])=O)C1=O



The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All
Tocris
products are intended for laboratory research use only.



Solubility Data




Solvent

Max Conc. mg/mL

Max Conc. mM



Solubility



DMSO

37.13

100





Preparing Stock Solutions

The following data is based on the
product
molecular weight
371.3
. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.



Concentration / Solvent Volume / Mass

1 mg

5 mg

10 mg



1 mM

2.69 mL

13.47 mL

26.93 mL



5 mM

0.54 mL

2.69 mL

5.39 mL



10 mM

0.27 mL

1.35 mL

2.69 mL



50 mM

0.05 mL

0.27 mL

0.54 mL






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Product Datasheets


Certificate of Analysis / Product Datasheet


Safety Datasheet

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References

References are publications that support the products'
BIOLOG
ical activity.


Yang

et al
(2007) Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res.
67
9472 PMID: 17909057


Mi

et al
(2009) Cancer preventative isothiocyanates induce selective degradation of cellular α- and β-tubulins by proteasomes. J.Biol.Chem.
284
17039 PMID: 19339240


Brahemi

et al
(2010) Homology modelling of human E1 ubiquitin activating enzyme. Lett.Drug Des.Discov.
7
57 PMID: 20396627




Keywords: PYR 41, supplier, PYR41, ubiquitin-activating, enzyme, E1, inhibitors, inhibits, ubiquitylation, post-translational, modifications, proteasomal, proteasome, sumoylation, sumo, ubiquitin, Ubiquitin-activating, Enzyme, E1, Post-translational, Modifications, Ubiquitin-activating, Enzyme, E1,
Tocris
Bioscience