| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CBP (CREB‑binding protein) bromodomain. By inhibiting the CBP bromodomain, Ischemin sodium prevents the interaction of CBP with acetylated histones and transcription factors such as p53, thereby reducing CBP‑mediated transcriptional activation.
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| ln Vitro |
Ischemin sodium (50, 100 µM; 24 h) inhibits p53 activation induced by DNA damage stress in U2OS cells[1]. Ischemin sodium (10 μM; 3 days) blocks cardiomyocyte apoptosis by inhibiting the activity of caspase 3/7[1]. Ischemin sodium salt inhibits the p53 signaling pathway in U2OS cells[1].
Ischemin sodium inhibits the p53‑CBP interaction, which leads to a reduction in p53 transcriptional activity. In cells, it decreases p53‑induced p21 activation with an IC50 of 5 uM. At a concentration of 50‑100 uM, it inhibits p53 activation induced by DNA damage stress in U2OS cells. Additionally, it has been shown to block doxorubicin‑induced apoptosis in cardiomyocytes, providing a protective effect. |
| ln Vivo |
In vivo, Ischemin sodium has demonstrated protective effects against ischemic injury. It is used in research to prevent apoptosis in ischemic cardiomyocytes, suggesting its potential as a cardioprotective agent in models of myocardial infarction and other ischemia‑related conditions.
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| Enzyme Assay |
A general cell‑free protocol for bromodomain inhibition uses a time‑resolved fluorescence resonance energy transfer (TR‑FRET) assay. Recombinant CBP bromodomain is incubated with a biotinylated acetylated histone H4 peptide and varying concentrations of Ischemin sodium (0.1‑100 uM). Europium‑labeled anti‑GST antibody and streptavidin‑XL665 are then added. The TR‑FRET signal is measured to calculate the IC50.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: U2OS Tested Concentrations: 50, 100 μM Incubation Duration: 24 h Experimental Results: Inhibited the Doxorubicin-induced increased levels of p53 protein, its Ser15-phosphorylated (p53S15p) and Lys382-acetylated (p53K382ac). Apoptosis Analysis[1] Cell Types: U2OS Tested Concentrations: 10 μM Incubation Duration: 3 days Experimental Results: Functioned as a cellular protective agent againsted myocardial ischemic stress. A general cellular protocol for Ischemin sodium involves treating U2OS or H9c2 cells with Ischemin sodium (1, 5, 10, 25, 50 uM) for 24 hours, followed by exposure to a DNA damage stressor (e.g., doxorubicin or hydrogen peroxide). Cell viability is assessed by MTT assay. Apoptosis is evaluated by measuring caspase‑3/7 activity, Annexin V/PI staining, and flow cytometry. p53 transcriptional activity is assessed using a luciferase reporter assay, and p21 protein levels are measured by Western blot. |
| Animal Protocol |
A general animal protocol for Ischemin sodium involves a mouse model of myocardial ischemia‑reperfusion injury. Mice are administered Ischemin sodium via intraperitoneal injection at doses of 1, 5, and 10 mg/kg, 30 minutes prior to inducing ischemia. The left anterior descending (LAD) artery is ligated for 30 minutes, followed by reperfusion for 24 hours. The infarct size is measured by TTC staining, and serum cardiac troponin I (cTnI) levels are assessed. Apoptosis in the heart tissue is evaluated by TUNEL staining and caspase‑3 activity assays.
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| ADME/Pharmacokinetics |
General PK protocol for Ischemin sodium: Ischemin sodium is a small, water‑soluble compound; a standard PK study in Sprague‑Dawley rats following IV (2 mg/kg) and oral (10 mg/kg) administration would be performed. Blood samples are collected at various time points, and plasma concentrations are analyzed by LC‑MS/MS. PK parameters (Cmax, Tmax, AUC, t1/2) are calculated.
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| Toxicity/Toxicokinetics |
General toxicity protocol: A 14‑day repeated‑dose toxicity study would be performed in ICR mice. Ischemin sodium would be administered intraperitoneally at doses of 5, 15, and 50 mg/kg/day. Parameters include clinical signs, body weight, hematology, serum chemistry, and histopathology of major organs, with special attention to the heart and liver.
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| References | |
| Additional Infomation |
Ischemin sodium is noted for its cell permeability and water solubility. It is also known as Ischemin sodium salt. The compound binds to the CBP bromodomain with a Kd of 19 uM. It is used as a research tool to study the role of CBP in transcription and apoptosis.
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| Molecular Formula |
C15H16N3NAO4S
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|---|---|
| Molecular Weight |
357.36
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| Appearance |
Solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O : 36 mg/mL (100.74 mM; with sonication and heat)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7983 mL | 13.9915 mL | 27.9830 mL | |
| 5 mM | 0.5597 mL | 2.7983 mL | 5.5966 mL | |
| 10 mM | 0.2798 mL | 1.3991 mL | 2.7983 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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