iKIX1

iKIX1

CAT N°: 19839
Price:

From 48.00 40.80

iKIX1 is an inhibitor of interactions between the transcription co-activator Mediator complex and the pleitropic drug resistance (CgPdr1) transcription factor in the pathogen C. glabrata.{48515} It inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 ?M). iKIX1 (10 and 30 ?M) inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata. It increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to the antifungal compounds fluconazole (Item No. 11594) and ketoconazole (Item No. 15212) in a concentration-dependent manner. iKIX1 (100 mg/kg) decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata when administered in combination with low and high doses of fluconazole, respectively.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-cyano-acetic acid, 2-[[(3,4-dichlorophenyl)amino]thioxomethyl]hydrazide
  • Correlated keywords
    • iKIX 1 coactivator CgPdr Candida CgGal 11A 11 A multi drug anti fungal
  • Product Overview:
    iKIX1 is an inhibitor of interactions between the transcription co-activator Mediator complex and the pleitropic drug resistance (CgPdr1) transcription factor in the pathogen C. glabrata.{48515} It inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 ?M). iKIX1 (10 and 30 ?M) inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata. It increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to the antifungal compounds fluconazole (Item No. 11594) and ketoconazole (Item No. 15212) in a concentration-dependent manner. iKIX1 (100 mg/kg) decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata when administered in combination with low and high doses of fluconazole, respectively.

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