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

506164
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₁H₁₁NO₃S₂ • HCl 1036069-26-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      506164-5MG
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          5 mg
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          Description
          OverviewA 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          506164

          References

          Reference overview
          Kravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA 105, 6302.
          Data Sheet

          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 +2°C to +8°C
          Hygroscopic
          Protect from light
          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.