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| Targets |
p-nitro-Pifithrin-alpha targets p53 by hindering its ability to bind to DNA, thereby interrupting p53-mediated transcriptional activation and subsequent apoptosis. It suppresses p53-dependent gene expression, including p53-mediated TGF-beta1 expression.
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| ln Vitro |
In cell-free systems, p-nitro-Pifithrin-alpha blocks p53-DNA binding, disrupting its transcriptional activity. It shows potent inhibition of p53 function with an ED50 of 30 nM for protecting cortical neurons from etoposide-induced apoptosis. The cyclic structure enhances potency compared to standard pifithrin-alpha.
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| ln Vivo |
In HK-2 kidney cells, p-nitro-Pifithrin-alpha (0.1-10 uM) effectively suppresses p53-mediated TGF-beta1 expression and prevents caspase-3 activation induced by various stress stimuli. It provides cytoprotection in neurons, kidney cells, and other cell types against p53-dependent apoptosis induced by DNA-damaging agents.
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| Enzyme Assay |
In cell-free p53-DNA binding assays, p-nitro-Pifithrin-alpha is incubated with recombinant p53 protein and a fluorescein-labeled DNA oligonucleotide containing the p53 consensus binding sequence. DNA binding is quantified by fluorescence polarization (FP) or electrophoretic mobility shift assay (EMSA). The reduction in binding at increasing compound concentrations indicates p53 inhibition.
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| Cell Assay |
Cells (e.g., HK-2, primary cortical neurons) are pre-treated with 0.1-10 uM p-nitro-Pifithrin-alpha for 1-2 hours before exposure to a p53-activating stimulus (e.g., etoposide, UV irradiation, doxorubicin). p53 target gene expression (p21, Bax, TGF-beta1) is quantified by qRT-PCR or Western blot. Apoptosis is assessed by caspase-3 activity and Annexin V staining.
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| Animal Protocol |
In rodent models of cerebral ischemia, neurotoxicity, or kidney injury, p-nitro-Pifithrin-alpha is administered intraperitoneally at 1-5 mg/kg 30-60 min before or after injury induction. p53 target gene expression is measured in target tissues. Functional outcomes (neurological scores, renal function markers) and tissue apoptosis (TUNEL, caspase-3 activation) are assessed to evaluate the protective effect against p53-mediated damage.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic studies are limited. p-nitro-Pifithrin-alpha is cell-permeable and expected to have improved in vivo stability compared to pifithrin-alpha. For in vivo use, it is typically formulated in DMSO/saline mixtures. The compound demonstrates brain penetration in rodent models.
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| Toxicity/Toxicokinetics |
Acute toxicity studies in rodents show a manageable safety profile at doses up to 10 mg/kg. Higher doses may cause gastrointestinal disturbances. p-nitro-Pifithrin-alpha is not approved for human use and is strictly for research applications. Standard safety precautions for laboratory chemicals should be followed.
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| References |
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| Additional Infomation |
This is a research-grade inhibitor, not an approved drug. It is useful for studying p53-mediated apoptosis, cell cycle regulation, DNA repair, and the molecular mechanisms underlying cell senescence and stress responses. Molecular formula: C15H15N3O3S•HBr; molecular weight: 398.27. Purity: ≥97%.
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| Molecular Formula |
C15H16BRN3O3S
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|---|---|
| Molecular Weight |
398.274841308594
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| Exact Mass |
397.009
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| CAS # |
389850-21-9
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| PubChem CID |
11553038
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
533
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NXPCMOGORSWOLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15N3O3S.BrH/c16-15-17(12-3-1-2-4-14(12)22-15)9-13(19)10-5-7-11(8-6-10)18(20)21;/h5-8,16H,1-4,9H2;1H
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| Chemical Name |
2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-nitrophenyl)ethanone;hydrobromide
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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, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5109 mL | 12.5543 mL | 25.1086 mL | |
| 5 mM | 0.5022 mL | 2.5109 mL | 5.0217 mL | |
| 10 mM | 0.2511 mL | 1.2554 mL | 2.5109 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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