iKIX1
Based on 1 Customer Validation
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.
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- Pureza: 99.76%
- No. CAS: 656222-54-7
- Fòrmula: C10H8Cl2N4OS
- Peso molecular:303.17
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 190.2 μM (interaction between CgGal11A and CgPdr1)Ki: 18 μM (interaction between CgGal11A and CgPdr1)[1]
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
100 μM
Compound: 92
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Cytotoxicity in human HepG2 cells
Cytotoxicity in human HepG2 cells
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[PMID: 29294275] |
iKIX1 (10-20 μg/ml) inhibits cell growth in a concentration-dependent manner in the presence of 5 µM ketoconazole (KET) in HepG2 cells[1].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[1]. 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[1].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[1]. 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[1]. 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 656222-54-7
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Appearance Solid
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Peso molecular 303.17
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Fòrmula C10H8Cl2N4OS
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Color Off-white to light yellow
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SMILES
O=C(NNC(NC1=CC=C(Cl)C(Cl)=C1)=S)CC#N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 83.33 mg/mL (274.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (6.86 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2985 mL | 16.4924 mL | 32.9848 mL | 82.4620 mL |
| 5 mM | 0.6597 mL | 3.2985 mL | 6.5970 mL | 16.4924 mL | |
| 10 mM | 0.3298 mL | 1.6492 mL | 3.2985 mL | 8.2462 mL | |
| 15 mM | 0.2199 mL | 1.0995 mL | 2.1990 mL | 5.4975 mL | |
| 20 mM | 0.1649 mL | 0.8246 mL | 1.6492 mL | 4.1231 mL | |
| 25 mM | 0.1319 mL | 0.6597 mL | 1.3194 mL | 3.2985 mL | |
| 30 mM | 0.1099 mL | 0.5497 mL | 1.0995 mL | 2.7487 mL | |
| 40 mM | 0.0825 mL | 0.4123 mL | 0.8246 mL | 2.0615 mL | |
| 50 mM | 0.0660 mL | 0.3298 mL | 0.6597 mL | 1.6492 mL | |
| 60 mM | 0.0550 mL | 0.2749 mL | 0.5497 mL | 1.3744 mL | |
| 80 mM | 0.0412 mL | 0.2062 mL | 0.4123 mL | 1.0308 mL | |
| 100 mM | 0.0330 mL | 0.1649 mL | 0.3298 mL | 0.8246 mL |
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