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4μ8C (Synonyms: 4u8C)

Catalog No.GC14493

IRE1 Rnase inhibitor, potent and non-toxic

Products are for research use only. Not for human use. We do not sell to patients.

4μ8C Chemical Structure

Cas No.: 14003-96-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$37.00
In stock
10mg
$74.00
In stock
50mg
$232.00
In stock
500mg
$618.00
In stock
1g
$927.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 14003-96-4 SDF
Synonyms 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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