506164

mutant p53 Reactivator, RETRA

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.

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₁H₁₁NO₃S₂ · xHCl
• CAS-Nummer: 1036069-26-7
• Molekulargewicht: 269.34 (free base basis)
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 100 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 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
• InChIKey: ZZAVDVMJZKDBIB-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Toxic (F)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable