产品
编 号：F601047
分子式：C10H8Cl2N4OS
分子量：303.17
分子式：C10H8Cl2N4OS
分子量：303.17
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是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 656222-54-7
产品详情
生物活性：
iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
体外研究：
iKIX1 (10-20 μg/ml)?inhibits cell growth in a concentration-dependent manner in the presence of 5 μM ketoconazole (KET) in HepG2 cells.FP titration curve showing the interaction of?CgGal11A KIX domain with?CgPdr1 AD30 fitted to a Kd?of 319.7 nM.?iKIX1?competes out?CgPdr1 AD30 with an IC50 of 190.2 μM . In vitro?binding studies, iKIX1 reveals that the Kd of the?CgPdr1 activation domain (AD) for the?CgGal11A KIX domain is 0.32 μM and the apparent Ki for?iKIX1?is 18 μM.iKIX1 (0-50 μM) 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 μM) 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.
iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
体外研究：
iKIX1 (10-20 μg/ml)?inhibits cell growth in a concentration-dependent manner in the presence of 5 μM ketoconazole (KET) in HepG2 cells.FP titration curve showing the interaction of?CgGal11A KIX domain with?CgPdr1 AD30 fitted to a Kd?of 319.7 nM.?iKIX1?competes out?CgPdr1 AD30 with an IC50 of 190.2 μM . In vitro?binding studies, iKIX1 reveals that the Kd of the?CgPdr1 activation domain (AD) for the?CgGal11A KIX domain is 0.32 μM and the apparent Ki for?iKIX1?is 18 μM.iKIX1 (0-50 μM) 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 μM) 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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