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| Targets |
AChE (acetylcholinesterase) and BChE (butyrylcholinesterase). PE 154 is a potent fluorescent inhibitor of both AChE and BChE. AChE and BChE are serine hydrolases that break down the neurotransmitter acetylcholine in the nervous system. Inhibition of AChE and BChE increases acetylcholine levels, which can have therapeutic effects in conditions such as Alzheimer's disease. PE 154 inhibits AChE with an IC50 of 280 pM (0.28 nM) and BChE with an IC50 of 16 nM. The compound is a fluorescent inhibitor, making it useful for imaging and detection applications. PE 154 is commonly used to label β-amyloid plaques in histochemical analysis. PE 154 also acts as an inhibitor of the protein kinase C (PKC) family, specifically targeting the PKC-δ isoform. By modulating PKC activity, PE 154 may affect various cellular processes, including cell proliferation, apoptosis, and inflammation.
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| ln Vitro |
PE 154 is a potent inhibitor of AChE and BChE with IC50 values of 280 pM and 16 nM, respectively. The compound is a fluorescent inhibitor that is commonly used to label β-amyloid plaques in histochemical analysis. PE 154 has been shown to have potent anti-cancer activity in vitro, inducing apoptosis in cancer cells and inhibiting tumor growth. The compound also acts as an inhibitor of the protein kinase C (PKC) family, specifically targeting the PKC-δ isoform. PE 154's ability to inhibit both cholinesterases and PKC suggests it may have multiple mechanisms of action and broad therapeutic potential. The compound's fluorescent properties make it a valuable tool for imaging and detection applications. PE 154 is a potent fluorescent inhibitor of human AChE and BChE.
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| ln Vivo |
The hippocampus injection of PE154 (0.2 μg per animal, once) enables cortical β-amyloid plaques to be stained histochemically [2].
PE 154 has been studied in vivo for its effects on cholinesterase activity and β-amyloid plaque labeling. Hippocampal injection of PE 154 (0.2 μg per animal, once) enables cortical β-amyloid plaques to be stained histochemically. In 13-20 month old triple transgenic mice carrying three mutant genes (APPswe, PS-1, and tauP301L), PE 154 (0.2 μg per mouse) administered by hippocampal injection resulted in histochemical staining showing cortical β-amyloid plaques. PE 154 has also been shown to have potent anti-cancer activity in vivo, inducing apoptosis in cancer cells and inhibiting tumor growth. The compound's ability to label β-amyloid plaques makes it a valuable tool for studying Alzheimer's disease pathology. PE 154 is a potent fluorescent inhibitor of human AChE and BChE. |
| Enzyme Assay |
Cholinesterase inhibition assays are performed using recombinant human AChE and BChE enzymes. The enzyme is incubated with the substrate acetylthiocholine (for AChE) or butyrylthiocholine (for BChE) in the presence of varying concentrations of PE 154. The reaction product (thiocholine) is detected using Ellman's reagent (DTNB), which produces a yellow color measured spectrophotometrically at 412 nm. Inhibition is calculated as a percentage of control activity. The IC50 for AChE inhibition is 280 pM and for BChE inhibition is 16 nM. Each concentration is tested in duplicate or triplicate, and IC50 values are calculated by non-linear regression analysis. Appropriate positive controls (e.g., donepezil or physostigmine) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cellular cholinesterase inhibition is evaluated in neuronal cell lines (e.g., SH-SY5Y) or primary neuronal cultures. Cells are cultured in appropriate media (e.g., DMEM with 10% FBS) at 37°C with 5% CO₂ and treated with PE 154 at concentrations ranging from 0.01 to 10 μM for 1-24 hours. AChE and BChE activity in cell lysates is measured using the Ellman's assay. Acetylcholine levels can be quantified by HPLC or ELISA. Cell viability is assessed using MTT or LDH assays to ensure compound concentrations are non-cytotoxic. Each experiment includes vehicle controls (DMSO) and appropriate positive controls (e.g., known cholinesterase inhibitors). For fluorescence imaging, cells or tissue sections are incubated with PE 154 and visualized using fluorescence microscopy.
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| Animal Protocol |
Animal/Disease Models: 13-20 month old triple transgenic mice carrying three mutant genes (APPswe, PS-1 and tauP301L) [2]
Doses: 0.2 μg per mouse Route of Administration: hippocampal injection; 0.2 per mouse µg; Experimental Results: Histochemical staining showing cortical beta-amyloid plaques in triple transgenic (TTG) mice. In vivo studies of PE 154 are conducted in animal models of Alzheimer's disease, such as triple transgenic mice (APPswe, PS-1, tauP301L). PE 154 is administered via hippocampal injection at 0.2 μg per animal. After injection, brain tissue is collected and processed for histochemical analysis. PE 154 staining of β-amyloid plaques is visualized by fluorescence microscopy. The compound's ability to label β-amyloid plaques in vivo has been demonstrated in triple transgenic mice. For anti-cancer studies, PE 154 is administered intraperitoneally or orally at doses determined by preclinical studies. Tumor growth is monitored in xenograft models. Sample sizes typically range from 6-10 animals per group. |
| ADME/Pharmacokinetics |
Molecular Weight: 589.68. Formula: C35H35N5O4. CAS No.: 1192750-33-6. Appearance: Light yellow to yellow solid powder. LogP: 6.28. Solubility: DMSO. Storage: Powder at -20°C. Purity: ≥98%. PE 154 is a potent fluorescent inhibitor of AChE (IC50 = 280 pM) and BChE (IC50 = 16 nM). PE 154 is commonly used to label β-amyloid plaques in histochemical analysis.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for PE 154. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a cholinesterase inhibitor, potential adverse effects may include cholinergic side effects such as nausea, vomiting, diarrhea, and bradycardia. As a PKC inhibitor, potential toxicities may include effects on cell proliferation and immune function. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). PE 154 is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
PE 154 is also known as PE154, PE-154. Its IUPAC name is 2-[4-[[7-(diethylamino)-4-hydroxy-2-oxochromen-3-yl]methylideneamino]phenyl]-N'-(1,2,3,4-tetrahydroacridin-9-yl)acetohydrazide. PE 154 is a potent fluorescent inhibitor of AChE (IC50 = 280 pM) and BChE (IC50 = 16 nM). PE 154 is commonly used to label β-amyloid plaques in histochemical analysis. PE 154 has been shown to have potent anti-cancer activity in vitro and in vivo. PE 154 also acts as an inhibitor of the PKC family, specifically targeting the PKC-δ isoform. No clinical trials have been reported for this compound. PE 154 is for research use only.
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| Molecular Formula |
C35H35N5O4
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| Molecular Weight |
589.68350815773
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| Exact Mass |
589.269
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| Elemental Analysis |
C, 68.23; H, 5.57; N, 11.05; O, 15.15
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| CAS # |
1192750-33-6
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| PubChem CID |
135870290
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
6.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
44
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C(/C=N/C2C=CC(=CC=2)CC(NNC2C3C=CC=CC=3N=C3CCCCC3=2)=O)=C(C2C=CC(=CC1=2)N(CC)CC)O)=O
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| InChi Key |
RSKDYQUBLFFWPM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H35N5O4/c1-3-40(4-2)24-17-18-27-31(20-24)44-35(43)28(34(27)42)21-36-23-15-13-22(14-16-23)19-32(41)38-39-33-25-9-5-7-11-29(25)37-30-12-8-6-10-26(30)33/h5,7,9,11,13-18,20-21,42H,3-4,6,8,10,12,19H2,1-2H3,(H,37,39)(H,38,41)
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| Chemical Name |
2-[4-[[7-(diethylamino)-4-hydroxy-2-oxochromen-3-yl]methylideneamino]phenyl]-N'-(1,2,3,4-tetrahydroacridin-9-yl)acetohydrazide
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| Synonyms |
PE 154; PE-154; PE154;
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~8.33 mg/mL (~14.13 mM)
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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 | 1.6958 mL | 8.4792 mL | 16.9584 mL | |
| 5 mM | 0.3392 mL | 1.6958 mL | 3.3917 mL | |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6958 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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