An inhibitor of interactions between the transcription co-activator Mediator complex and the CgPdr1 transcription factor in the pathogen C. glabrata; inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 μM); inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata at 10 and 30 μM; increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to fluconazole and ketoconazole; decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata at 100 mg/kg when administered in combination with low and high doses of fluconazole

iKIX1 – 1 mg

Brand:
Cayman
CAS:
656222-54-7
Storage:
-20
UN-No:
Non-Hazardous - /

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 μM). iKIX1 (10 and 30 μM) 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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Description

An inhibitor of interactions between the transcription co-activator Mediator complex and the CgPdr1 transcription factor in the pathogen C. glabrata; inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 μM); inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata at 10 and 30 μM; increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to fluconazole and ketoconazole; decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata at 100 mg/kg when administered in combination with low and high doses of fluconazole, respectively

Formal name: 2-cyano-acetic acid, 2-[[(3,4-dichlorophenyl)amino]thioxomethyl]hydrazide

Synonyms: 

Molecular weight: 303.2

CAS: 656222-54-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Fungal Diseases|Candidiasis

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