[CAS NO. 1043854-13-2]  J14

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PRODUCTS SPECIFICATIONS [1043854-13-2]

Catalog
HY-135008
Brand
MCE
CAS
1043854-13-2

DESCRIPTION [1043854-13-2]

Overview

MDLMFCD19814303
Molecular Weight517.04
Molecular FormulaC28H25ClN4O2S
SMILESO=C(O)C1=CC=C(CSC2=NC(C3=CC=CC=C3)=CC(N4CCN(C5=CC=CC=C5Cl)CC4)=N2)C=C1

For research use only. We do not sell to patients.

Summary

J14 is a reversible sulfiredoxin inhibitor with an IC 50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin , leading to cytotoxicity and cancer cell death [1] .


IC50 & Target

IC50: 8.1 μM (Sulfiredoxin); ROS [1]


In Vitro

J14 (0-100 μM; 0-96 hours; A549 cells) treatment inhibits the growth of A549 cells in a concentration- and a time- dependent manner, and its half inhibitory concentration for the growth of A549 cells was 15.7 μM [1] .
J14 (20 μM; 48-72 hours; A549 cells) treatment causes not only the release of cytochrome c into the cytosol, but also the activation of caspase-3 and caspase-9. J14 induces oxidative damage to mitochondria, resulting in caspase-mediated apoptosis [1] .
J14 treatment significantly increases the accumulation of sulfinic peroxiredoxins and intracellular ROS. Excess accumulation of intracellular ROS causes oxidative damage, leading to cell death. J14 significantly induces cell death in A549 cells in a time-dependent manner, resulting in approximately 40% cell death in 96 hours [1] .
J14 induces oxidative mitochondrial damage and apoptosis [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay [1]

Cell Line: A549 cells
Concentration: 0-100 μM
Incubation Time: 0 hour, 24 hours, 48 hours, 72 hours, 96 hours
Result: Inhibited the growth of A549 cells in a concentration- and a time- dependent manner.

Western Blot Analysis [1]

Cell Line: A549 cells
Concentration: 20 μM
Incubation Time: 48 hours, 72 hours
Result: Caused not only the release of cytochrome c into the cytosol, but also the activation of caspase-3 and caspase-9.

In Vivo

J14 (50 mg/kg; intraperitoneal injection; daily; for 16 days; BALB/c nude female mice) treatment significantly reduces the average tumor volume. The masses and weights of the primary tumors excised from the J14-treated mice are significantly lower compared with those of the control mice [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old BALB/c nude female mice injected with A549 cells [1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; daily; for 16 days
Result: Significantly reduced the growth of human lung tumor without acute toxicity.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01820780 Assistance Publique - Hôpitaux de Paris
Heart Failure
June 10, 2013 Not Applicable

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL ( 241.76 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9341 mL 9.6704 mL 19.3409 mL
5 mM 0.3868 mL 1.9341 mL 3.8682 mL
10 mM 0.1934 mL 0.9670 mL 1.9341 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.17 mg/mL (4.20 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.20 mM); Clear solution

* All of the co-solvents are available by MCE.