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iKIX1

CAS No. : 656222-54-7

MCE 站：iKIX1

产品活性：iKIX1 是一种抗真菌剂 (antifungal agent)，可在体外使耐药的光滑毛囊念珠菌对唑类抗真菌剂重新敏感。iKIX1 抑制介体亚基 CgGal11A 的 KIX 结构域与 CgPdr1 的激活结构域之间的相互作用，IC₅₀ 和 K_i 分别为 190.2 μM 和 18 μM。iKIX1 用于研究多药耐药性和光滑念珠菌感染。

研究领域：Anti-infection

作用靶点：Fungal

In Vitro: iKIX1 (10-20 μg/ml)?inhibits cell growth in a concentration-dependent manner in the presence of 5 ?M ketoconazole (KET) in HepG2 cells.
FP titration curve showing the interaction of?CgGal11A KIX domain with?CgPdr1 AD30 fitted to a K_d?of 319.7 nM.?iKIX1?competes out?CgPdr1 AD30 with an IC₅₀ of 190.2 ?M . In vitro?binding studies, iKIX1 reveals that the K_d of the?CgPdr1 activation domain (AD) for the?CgGal11A KIX domain is 0.32 ?M and the apparent K_i for?iKIX1?is 18 ?M.
iKIX1 (0-50 ?M) inhibits Ketoconazole (KET)-induced upregulation of luciferase activity in a dose-responsive manner in a?Sc pdr1Δpdr3Δ?strain containing plasmid-borne?CgPDR1?and 3XPDRE-luciferase.
A chromatin immunoprecipitation (ChIP) assay is used to examine Gal11/Med15 recruitment to Pdr1-regulated target genes in?S. cerevisiae. Ketoconazole induces Gal11/Med15 rapidly recruited to the promoters of the Pdr1 target genes?PDR5?and?SNQ2. iKIX1 abrogates Ketoconazole-induced recruitment of Gal11/Med15 and strongly inhibits azole-induced transcription of?ScPdr1 target genes.
iKIX1?(20 μM) has an effect on the transcription of?C. glabrata?Pdr1-regulated genes involved in drug efflux and MDR (CgCDR1, CgCDR2?and?CgYOR1).?iKIX1?alone does not significantly affect Pdr1-target gene induction. But pre-treatment with iKIX1?reduces ketoconazole-induced CgPdr1 up-regulation in a durable and concentration-dependent manner.
In RNA sequencing (RNA-Seq) assay of a?C. glabrata SFY114 (PDR1?wild-type) strain.?Azole up-regulates Pdr1-dependent genes in both yeasts, such as the drug efflux pumps?ScPDR5?and?CgCDR1i. KIX1?combines azole strongly blunts expression of many azole-activated and Pdr1-dependent genes in both?S.cerevisiae?and?C. glabrata, but iKIX1?alone affects very different sets of genes in?S.cerevisiae?and?C. glabrata. And then iKIX1?does not significantly alter the expression of?PDR1?or?GAL11/MED15 affects very different sets of genes in?S.cerevisiae and?C. glabrata. iKIX1?(0-150 ?M) restores the efficacy of azoles towards?CgPDR1?gain-of-function mutants. It restores azole-sensitivity to?PDR1?gain-of-function mutant strains in a concentration-dependent manner.

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