4μ8C (Synonyms: 4u8C) |
| Catalog No.GC14493 |
Inhibidor de la Rnasa IRE1, potente y no tóxico.
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.
The inositol-requiring enzyme 1α (IRE1α) is a serine-threonine kinase that plays crucial roles in activating the unfolded protein response. Studies suggest that IRE1α is activated during thymic T cell development and in effector CD8+ T cells. 4μ8C is a potent and selective IRE1 Rnase inhibitor.
In vitro: 4μ8c is a potent and non-toxic inhibitor of IRE1 RNase activation in response to both hypoxia and other ER stress-inducing agents. This compound effectively inhibited IRE1 induced activation of the downstream target genes in both HCT116 colorectal cancer and KP4 pancreatic cancer cell lines under hypoxia. However, despite potent inhibition of IRE1 activation and the, 4μ8c had no effect on cell proliferation or clonogenic survival of HCT116 and KP4 cells during exposure to hypoxia or anoxia. Similarly, 4μ8c inhibition of IRE1 did not sensitize cells to other ER stress inducing agents [1].
In vivo: 4μ8C has not been tested in vivo, probably because of its unfavourable pharmacokinetics.
Clinical trial: Up to now, 4μ8C is still in the preclinical development stage.
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 | |
| Sinónimos | 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 |
| Solubility | ≥ 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. |
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| 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)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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