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商品編號


2443/1



品牌


Tocris



公司


Bio-Techne Corporation



公司分類(lèi)


Ligases



Size

1 mg

商品信息

Description:
MDM2-p53 interaction inhibitor

Alternative Names:
NSC 652287

Chemical Name:
5,5'-(2,5-Furandiyl)
bis
-2-thiophenemethanol

Purity:
≥97% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Anti-tumor agent that binds wild-type p53 (K
d
= 1.5 nM) preventing p53-MDM2 (HDM2) interaction. Induces p53 accumulation and stimulates apoptosis in tumor cell lines expressing wild-type p53
in vitro
and
in vivo
. Inhibits HPV-E6-mediated proteasomal degradation. Suppresses expression of cervical carcinoma HeLa xenografts
in vivo
.



Technical Data



M. Wt

292.37



Formula

C
14
H
12
O
3
S
2




Storage

Store at -20°C



Purity

≥97% (HPLC)



CAS Number

213261-59-7



PubChem ID

374536



InChI Key

KZENBFUSKMWCJF-UHFFFAOYSA-N



Smiles

OCC1=CC=C(S1)C1=CC=C(O1)C1=CC=C(CO)S1



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

29.23

100



ethanol

7.31

25





Preparing Stock Solutions

The following data is based on the
product
molecular weight
292.37
. 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

3.42 mL

17.1 mL

34.2 mL



5 mM

0.68 mL

3.42 mL

6.84 mL



10 mM

0.34 mL

1.71 mL

3.42 mL



50 mM

0.07 mL

0.34 mL

0.68 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.


Rivera

et al
(1999) Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism. Biochem.Pharmacol.
57
1283 PMID: 10230772


Zhao

et al
(2010) Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res.
70
3372 PMID: 20395210


Issaeva

et al
(2004) Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumours. Nature Med.
10
1321 PMID:


Espinoza-Fonseca
(2005) Targeting MDM2 by the small molecule RITA: towards the development of new multi-target drugs against cancer. Theor.Biol.Med.Mod.
2
38 PMID:




Keywords: RITA, supplier, p53-MDM2, interaction, inhibitors, inhibits, antitumor, agent, MDM2-p53, MDM2, p14ARF, p53, Ligases, Transcription, Factors, NSC652287, NSC, 652287, p53, Ubiquitin, E3, Ligases, Ubiquitin, E3, Ligases,
Tocris
Bioscience