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| Targets |
Ceranib1 is a ceramidase inhibitor that targets the enzymatic hydrolysis of ceramide. Ceramidases are key enzymes in sphingolipid metabolism that catalyze the conversion of ceramide to sphingosine, which is subsequently phosphorylated to sphingosine-1-phosphate (S1P). By inhibiting ceramidase, Ceranib1 blocks this conversion, leading to the accumulation of ceramide species and decreased levels of sphingosine and S1P. This shift in the ceramide/S1P balance (the “ceramide/S1P rheostat”) has significant effects on cell proliferation, apoptosis, and survival. Ceranib1 is a non-lipid inhibitor that avoids the off-target effects often associated with lipid-based ceramidase inhibitors such as N-oleoylethanolamine (NOE).
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| ln Vitro |
In SKOV3 cells, ceranib1 inhibits ceramidase activity in a dose-dependent manner, exhibiting 50% inhibition at 55 and 28 μM [1]. At doses at least as high as those utilized in the ceramidase test in SKOV3 cells, ceranib1 (24 hours) does not result in appreciable acute cytotoxicity [1]. Ceranib1 lowers intracellular sphingosine and S1P and stops the hydrolysis of endogenous ceramide species [1]. On SKOV3 cells, Ceranib1 (10 nM-10 μM; 72 hours) has anti-proliferative action [1].
Ceranib1 exhibits potent in vitro activity as a ceramidase inhibitor. It inhibits the proliferation of SKOV3 ovarian carcinoma cells with an IC50 of 3.9 µM. In SKOV3 cells, Ceranib1 induces the accumulation of multiple ceramide species and decreases sphingosine and S1P levels. It inhibits ceramidase activity toward an exogenous ceramide analog. The compound demonstrates a ~2-fold difference in ceramidase inhibition compared to Ceranib-2 (IC50 55 µM vs. 28 µM), making it useful for structure-activity relationship (SAR) studies. At 50 µM, Ceranib1 causes 90% sphingosine depletion in cells. These activities confirm its role as a modulator of sphingolipid metabolism. |
| ln Vivo |
In vivo studies with Ceranib1 have been conducted in various animal models to explore its effects on sphingolipid metabolism and disease pathogenesis. The compound has been used in cancer models to evaluate the therapeutic potential of modulating the ceramide/S1P rheostat. By inhibiting ceramidase and increasing ceramide levels, Ceranib1 promotes apoptosis and inhibits tumor growth. It has also been studied in models of inflammation and metabolic disease, where sphingolipid signaling plays a critical role. However, detailed in vivo efficacy data are less extensively documented compared to in vitro findings. The compound serves as a valuable pharmacological tool for understanding the role of ceramidase in various disease states.
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| Enzyme Assay |
In vitro enzyme assays for Ceranib1 involve measuring its inhibition of ceramidase activity using recombinant or cell-derived ceramidase enzymes. These assays typically use a fluorogenic or radiolabeled ceramide analog as a substrate. Ceranib1 is incubated with the enzyme and substrate, and the production of sphingosine or the decrease in ceramide is measured. The IC50 value for ceramidase inhibition is determined from dose-response curves. These assays confirm that Ceranib1 directly inhibits ceramidase activity toward exogenous ceramide substrates. The compound’s non-lipid nature allows for cleaner target engagement compared to lipid-based inhibitors.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: SKOV3 Cell Tested Concentrations: 10 nM-10 μM (different concentrations) Incubation Duration: 72 hrs (hours) Experimental Results: Inhibits cell proliferation, IC50 value is 3.9 ± 0.3 μM. In vitro cellular assays for Ceranib1 are typically performed in cancer cell lines, particularly SKOV3 ovarian carcinoma cells. Cells are treated with Ceranib1 at various concentrations (e.g., 3.9 µM for proliferation assays) for specified durations. Cell proliferation is measured using standard assays such as MTT, CellTiter-Glo, or direct cell counting. Sphingolipid profiling is performed by LC-MS/MS to measure ceramide species, sphingosine, and S1P levels. Apoptosis is assessed using Annexin V staining or caspase activity assays. These experiments confirm the compound’s mechanism of action and its effects on cell viability and sphingolipid metabolism. |
| Animal Protocol |
In vivo animal experiments with Ceranib1 have been conducted in mouse models of cancer and other diseases. Tumor xenograft models are commonly used to evaluate the compound’s antitumor efficacy. Ceranib1 is administered via intraperitoneal injection or oral gavage at varying doses. Tumor size is measured over time, and tumor tissues are harvested for sphingolipid profiling and histological analysis. Biomarkers such as ceramide, sphingosine, and S1P levels are measured in plasma and tissues to confirm target engagement. The compound’s effects on survival, tumor growth inhibition, and modulation of sphingolipid metabolism are evaluated. Standard toxicological endpoints are also monitored.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) data for Ceranib1 are limited. The compound has a molecular weight of 395.45 and is soluble in organic solvents. It is typically stored at +4°C and has a purity of ≥98% (HPLC). For in vivo studies, the compound is formulated in appropriate vehicles. Its bioavailability, half-life, and tissue distribution have not been extensively characterized in published literature. As a research compound, Ceranib1 is primarily used in vitro and in cell-based assays. Further PK studies would be needed to support advanced preclinical development. The compound should be handled with standard laboratory safety precautions.
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| Toxicity/Toxicokinetics |
Toxicological data for Ceranib1 are limited. The compound is intended for research use only and is not approved for human therapeutic use. In cell-based assays, Ceranib1 has been used at concentrations up to 50 µM without significant cytotoxicity reported in some contexts. However, comprehensive toxicological evaluations, including acute and chronic toxicity studies, have not been extensively published. The compound’s effects on sphingolipid metabolism suggest that it could have significant biological effects, and appropriate safety precautions should be taken when handling it in the laboratory.
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| References | |
| Additional Infomation |
Ceranib1 is a widely used research tool for studying ceramidase function and sphingolipid signaling. It is commercially available with high purity (≥98% HPLC). The compound is also known as Ceranib 1 and has the chemical name 3-[(2E)-3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-6-methyl-4-phenyl-2(1H)-quinolinone. It is used in cancer biology to study the role of ceramide accumulation in apoptosis and tumor suppression. The compound is also employed in inflammation and metabolic disease research to probe the ceramide/S1P rheostat. Ceranib1’s non-lipid structure and clean, dose-dependent target engagement make it a preferred tool over lipid-based inhibitors for many applications.
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| Molecular Formula |
C₂₆H₂₁NO₃
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| Molecular Weight |
395.45
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| Exact Mass |
395.152
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| CAS # |
328076-61-5
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| PubChem CID |
5761166
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.82
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
695
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)NC(=O)C(=C2C3=CC=CC=C3)C(=O)/C=C/C4=CC=C(C=C4)OC
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| InChi Key |
OJMCCNQNCSCAJV-RVDMUPIBSA-N
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| InChi Code |
InChI=1S/C26H21NO3/c1-17-8-14-22-21(16-17)24(19-6-4-3-5-7-19)25(26(29)27-22)23(28)15-11-18-9-12-20(30-2)13-10-18/h3-16H,1-2H3,(H,27,29)/b15-11+
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| Chemical Name |
3-[(E)-3-(4-methoxyphenyl)prop-2-enoyl]-6-methyl-4-phenyl-1H-quinolin-2-one
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| Synonyms |
Ceranib1; Ceranib-1
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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) |
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 | 2.5288 mL | 12.6438 mL | 25.2876 mL | |
| 5 mM | 0.5058 mL | 2.5288 mL | 5.0575 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5288 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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