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506164

mutant p53 Reactivator, RETRA

Name: mutant p53 Reactivator, RETRA
Brand: MM

The mutant p53 Reactivator, RETRA, also referenced under CAS 1036069-26-7, controls the biological activity of mutant p53. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

别名:

mutant p53 Reactivator, RETRA, p53 Activator VI, p73 Activator, 2-(4,5-Dihydro-1,3-thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanone, HCl, Reactivation of Transcriptional Reporter Activity

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关于此项目

经验公式（希尔记法）:

C₁₁H₁₁NO₃S₂ · xHCl

化学文摘社编号:

1036069-26-7

分子量:

269.34 (free base basis)

UNSPSC Code:

12352200

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, desiccated (hygroscopic), protect from light

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属性

Quality Level

100

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C11H11NO3S2.ClH/c13-8-2-1-7(5-9(8)14)10(15)6-17-11-12-3-4-16-11;/h1-2,5,13-14H,3-4,6H2;1H

InChI key

ZZAVDVMJZKDBIB-UHFFFAOYSA-N

说明

General description

A cell-permeable thioethanone compound that upregulates p53 family-responsive element-dependent reporter plasmid transcription activity in cells bearing Glu266, His273, Lys280, or Trp278 mutant p53 by increasing the cellular protein, but not mRNA, level of the p53 homologue p73 (by ~3.7-fold in A431 cells in 20 h with 2 µg/ml RETRA) as well as by disrupting p73 interaction with mutant p53, while exhibiting no similar effects in wild-type p53-bearing or p53-null cells. RETRA is shown to increase transcription of proapoptotic genes (5- and >10-fold increase, respectively, of PUMA/BBC3 and p21/CDKN1A, with 1.5 µg/ml RETRA for 14 h), induce apoptosis, and inhibit the growth of A431, but not wild-type p53-bearing or p53-null cells, in a p53- and p73-dependent manner in vitro, as well as delay (by ~4 days) and reduce (by ~50% on day 25) A431-derived tumor formation in mice (0.4 mg/animal via 6 daily i.p.) in vivo.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Kravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA105, 6302.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Toxic (F)

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c