iKIX1
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $600 | Check With Us |
| 200mg | $900 | Check With Us |
| 500mg | $1510 | Check With Us |
: Cat #: V22462 CAS #: 656222-54-7 Purity ≥ 98%
Description: iKIX1 is a novel and potent inhibitor of Pdr1-dependent gene activation with antifungal activity.
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| Molecular Weight (MW) | 303.17 |
|---|---|
| Molecular Formula | C10H8Cl2N4OS |
| CAS No. | 656222-54-7 |
| SMILES Code | O=C(NNC(NC1=CC=C(Cl)C(Cl)=C1)=S)CC#N |
| Synonyms | iKIX 1; iKIX1; iKIX-1; |
| Protocol | In Vitro | 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. iKIX1 (10-20 μg/ml) inhibits cell growth in a concentration-dependent manner in the presence of 5 µM ketoconazole (KET) in HepG2 cells. 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. 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[1]. 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. |
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These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.2985 mL | 16.4924 mL | 32.9848 mL | 65.9696 mL |
| 5mM | 0.6597 mL | 3.2985 mL | 6.5970 mL | 13.1939 mL |
| 10mM | 0.3298 mL | 1.6492 mL | 3.2985 mL | 6.5970 mL |
| 20mM | 0.1649 mL | 0.8246 mL | 1.6492 mL | 3.2985 mL |
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