4μ8C (Synonyms: 4u8C) |
Katalog-Nr.GC14493 |
IRE1 Rnase-Inhibitor, potent und ungiftig
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 14003-96-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Das Inositol-erforderliche Enzym 1α (IRE1α) ist eine Serin-Threonin-Kinase, die entscheidende Rollen bei der Aktivierung der ungefalteten Proteinantwort spielt. Studien legen nahe, dass IRE1α während der Entwicklung von Thymus-T-Zellen und in Effektor-CD8+-T-Zellen aktiviert wird. 4μ8C ist ein potenter und selektiver IRE1-Rnase-Inhibitor.
In vitro: 4μ8c ist ein wirksamer und ungiftiger Inhibitor der IRE1 RNase-Aktivierung als Reaktion auf sowohl Hypoxie als auch andere ER-Stress-induzierende Mittel. Dieses Verbindungsmittel hemmte effektiv die durch IRE1 induzierte Aktivierung von Zielgenen in beiden HCT116 Darmkrebs- und KP4 Bauchspeicheldrüsenkrebszelllinien unter Hypoxie. Trotz einer starken Hemmung der IRE1-Aktivierung hatte 4μ8c jedoch keinen Einfluss auf die Zellproliferation oder das klonogene Überleben von HCT116- und KP4-Zellen während der Exposition gegenüber Hypoxie oder Anoxie. Ebenso sensibilisierte die Hemmung von IRE1 durch 4μ8c die Zellen nicht für andere ER-Stress-induzierende Mittel [1].
In vivo: 4μ8C wurde wahrscheinlich aufgrund seiner ungünstigen Pharmakokinetik nicht in vivo getestet.
Klinische Studie: Bislang befindet sich 4μ8C noch in der präklinischen Entwicklungsphase.
Reference:
[1] Dan Cojocari, Ravi Vellanki, Brandon Sit, Marianne Koritzinsky, and Bradly G. Wouters. IRE1 and PERK as targets of cellular adaptation and survival to hypoxia. Mol Cancer Ther 2013;12(11 Suppl):C284.
[2] Hetz C, Chevet E, Harding HP. Targeting the unfolded protein response in disease. Nat Rev Drug Discov. 2013 Sep;12(9):703-19.
Cas No. | 14003-96-4 | SDF | |
Überlieferungen | 4u8C | ||
Chemical Name | 7-hydroxy-4-methyl-2-oxochromene-8-carbaldehyde | ||
Canonical SMILES | CC1=CC(=O)OC2=C1C=CC(=C2C=O)O | ||
Formula | C11H8O4 | M.Wt | 204.18 |
Löslichkeit | ≥ 8.65mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.8976 mL | 24.4882 mL | 48.9764 mL |
5 mM | 0.9795 mL | 4.8976 mL | 9.7953 mL |
10 mM | 0.4898 mL | 2.4488 mL | 4.8976 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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