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mutant p53 Reactivator, RETRA
2-(4,5-Dihydro-1,3-thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanone, HCl, Reactivation of Transcriptional Reporter Activity, p53 Activator VI, p73 Activator
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.
产品信息
Form Off-white solid
Molar mass 305.8
Protect from Light 是的
Hygrocopic 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C11H11NO3S2 • HCl
CAS number 1036069-26-7
商店和运输信息
Hazardous Materials Attention: Due to the nature of the Hazardous Materials in this shipment, additional shipping chargesmay 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
Ship Ambient Temperature Only
Toxic |