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506164 mutant p53 Reactivator, RETRA - CAS 1036069-26-7 - Calbiochem

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.

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Synonyme: 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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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      1036069-26-7C₁₁H₁₁NO₃S₂ • HCl
      Description
      Overview

      This product has been discontinued.



      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.
      Catalogue Number506164
      Brand Family Calbiochem®
      Synonymsp53 Activator VI, p73 Activator, 2-(4,5-Dihydro-1,3-thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanone, HCl, Reactivation of Transcriptional Reporter Activity
      References
      ReferencesKravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 6302.
      Product Information
      CAS number1036069-26-7
      FormOff-white solid
      Hill FormulaC₁₁H₁₁NO₃S₂ • HCl
      Chemical formulaC₁₁H₁₁NO₃S₂ • HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 25

      Toxic if swallowed.
      S PhraseS: 24/25-36/37/39-45

      Avoid contact with skin and eyes.
      Wear suitable protective clothing, gloves and eye/face protection.
      In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Toxic
      Hazardous Materials Attention: 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.
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      506164 0

      Documentation

      mutant p53 Reactivator, RETRA - CAS 1036069-26-7 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      mutant p53 Reactivator, RETRA - CAS 1036069-26-7 - Calbiochem Analysenzertifikate

      TitelChargennummer
      506164

      Literatur

      Übersicht
      Kravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 6302.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision22-April-2010 RFH
      Synonymsp53 Activator VI, p73 Activator, 2-(4,5-Dihydro-1,3-thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanone, HCl, Reactivation of Transcriptional Reporter Activity
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1036069-26-7
      Chemical formulaC₁₁H₁₁NO₃S₂ • HCl
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Toxicity Toxic
      ReferencesKravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 6302.