| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
I-152 activates NRF2 and ATF4 signaling pathways, which are involved in oxidative stress response and cellular defense mechanisms.
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|---|---|
| ln Vitro |
In RAW 264.7 cells, I-152 (1 mM; 1 h or 2 h) lowers NRF2 mRNA levels [1]. In RAW 264.7 cells, I-152 (1 mM; 0–60 min) decreases p53 and NRF2 levels while upregulating ATF4 expression [1]. The levels of Gclc mRNA (6 h or 24 h), Chac1 mRNA (6 h or 24 h), and Chop mRNA (6 h) in RAW 264.7 cells are increased by I-152 (0.062, 0.125, 0.25, or 1 mM)[1]. In RAW 264.7 cells, I-152 (0.062, 0.125, 0.25, or 1 mM; 2 h) raises GSH levels [1]. In RAW 264.7 cells, I-152 (1 mM; 1, 2, 6 and 24 h) stimulates the expression of ATF4 mRNA [1]. On RAW 264.7 cells, I-152 (1 mM; 24 h and 48 h) demonstrates growth inhibitory and cytotoxic effects [1].
In vitro, I-152 has anti-proliferative, antiviral, and immunomodulatory activities. It activates NRF2 and ATF4 signaling, leading to increased expression of antioxidant and cytoprotective genes. |
| ln Vivo |
In vivo, I-152 has shown activity in animal models of viral infections and oxidative stress-related diseases. It is being investigated for its potential to modulate oxidative stress and immune responses.
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| Enzyme Assay |
A non-cell assay for NRF2 activation is performed using a luciferase reporter gene. Cells are transfected with an ARE-luciferase reporter, then incubated with I-152. Luciferase activity is measured after 6-24 hours.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: RAW 264.7 cells. Tested Concentrations: 0.062, 0.125, 0.25, 1, 5 or 10 mM. Incubation Duration: 2 h or 24 h. Experimental Results: decreased the expression of NRF2/β-ACTIN, increased the expression of GCLM. For cell studies, I-152 is dissolved in DMSO or water and diluted in culture medium. Cells are treated for 4-24 hours. NRF2 target gene expression (NQO1, HMOX1) is measured by qPCR. Cell viability is measured by MTT assay for anti-proliferative activity. |
| Animal Protocol |
In animal studies, I-152 is typically administered to rodents by oral gavage or intraperitoneal injection. It is used in models of viral infection, oxidative stress, and inflammation. Tissue samples are collected to measure oxidative stress markers and cytokine levels.
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| ADME/Pharmacokinetics |
Limited PK data are available. The compound is expected to be metabolized to its constituent parts (NAC and cysteamine), which have well-characterized PK properties. Both are rapidly absorbed and have short half-lives.
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| Toxicity/Toxicokinetics |
The components NAC and cysteamine have well-established safety profiles. I-152 is generally well-tolerated at research doses. No significant toxicity has been reported.
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| References | |
| Additional Infomation |
I-152 is a research tool for studying NRF2 and ATF4 signaling pathways. It has potential therapeutic applications for viral infections, oxidative stress-related diseases, and as an immunomodulatory agent. It is not an approved drug.
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| Molecular Formula |
C9H16N2O3S2
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|---|---|
| Molecular Weight |
264.36
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| Exact Mass |
264.06
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| CAS # |
311343-11-0
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| PubChem CID |
484333
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| Appearance |
White to off-white solid powder
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| LogP |
1.497
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
16
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| Complexity |
272
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)N[C@@H](CS)C(=O)NCCSC(=O)C
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| InChi Key |
PCFWUYJHCYCQKP-QMMMGPOBSA-N
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| InChi Code |
InChI=1S/C9H16N2O3S2/c1-6(12)11-8(5-15)9(14)10-3-4-16-7(2)13/h8,15H,3-5H2,1-2H3,(H,10,14)(H,11,12)/t8-/m0/s1
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| Chemical Name |
S-[2-[[(2R)-2-acetamido-3-sulfanylpropanoyl]amino]ethyl] ethanethioate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~189.1 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1.25 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7827 mL | 18.9136 mL | 37.8272 mL | |
| 5 mM | 0.7565 mL | 3.7827 mL | 7.5654 mL | |
| 10 mM | 0.3783 mL | 1.8914 mL | 3.7827 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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