商品编号


6302



品牌


Tocris



公司


Bio-Techne Corporation



公司分类


Ligases



Size

10 mg

商品信息

Description:
Cereblon ubiquitination inhibitor; also TNF-α inhibitor and antiangiogenic

Chemical Name:
4-Amino-2-(2,6-dioxo-3-piperidinyl)-1
H
-isoindole-1,3(2
H
)-dione

Purity:
≥98% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Potent TNF-α inhibitor (IC
50
= 13 nM). Also potently inhibits IL-2 (EC
50
= 8 nM). Thalidomide derivative. Binds cereblon and inhibits its ubiquitination. Exhibits antiproliferative effects in a Namalwa lymphoma cell line. Antiangiogenic.



Technical Data



M. Wt

273.24



Formula

C
13
H
11
N
3
O
4




Storage

Store at +4°C



Purity

≥98% (HPLC)



CAS Number

19171-19-8



PubChem ID

134780



InChI Key

UVSMNLNDYGZFPF-UHFFFAOYSA-N



Smiles

NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=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

27.32

100





Preparing Stock Solutions

The following data is based on the
product
molecular weight
273.24
. 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

3.66 mL

18.3 mL

36.6 mL



5 mM

0.73 mL

3.66 mL

7.32 mL



10 mM

0.37 mL

1.83 mL

3.66 mL



50 mM

0.07 mL

0.37 mL

0.73 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.


Lohbeck & Miller
(2016) Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development. Bioorg.Med.Chem.Lett.
26
5260 PMID: 27687673


Nanthakumar

et al
(2015) Dissecting fibrosis: therapeutic insights from the small-molecule toolbox. Nat.Rev.Drug.Discov.
14
693 PMID: 26338155


Lai

et al
(2016) Modular PROTAC design for the degradation of oncogenic BCR-ABL. Angew.Chem.Int.Ed.Engl.
55
807 PMID: 26593377


Winter

et al
(2015) Phthalimide conjugation as a strategy for
in vivo
target protein degradation. Science.
348
1376 PMID: 5999370




Keywords: Pomalidomide, supplier, Pomalidomide, TNFa, TNFalpha, TNFα, Inhibitors, inhibits, IL-2, thalidomide, cereblon, binder, ubiquitination, antiproliferative, antiangiogenic, lymphoma, Ubiquitin, E3, Ligases,
Tocris
Bioscience