| Size | Price | Stock | Qty |
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| Targets |
CGP 53353 targets protein kinase C beta II (PKCβII), a serine-threonine kinase involved in various signaling pathways, including cell proliferation, differentiation, and apoptosis. It is a selective inhibitor of PKCβII with an IC50 of 0.41 μM. The compound also inhibits PKCβI with lower potency (IC50 = 3.8 μM).
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| ln Vitro |
In A10 cells, CGP-53353 (DAPH-7) (1 μM; 48-96 hours) inhibits the proliferation of cells induced by glucose [1]. The glucose-induced increase and acceleration of DNA synthesis in A10 is inhibited by CGP-53353 (1 μM; 0-48 hours), and it also prevents the glucose-induced increase in the percentage of cells in S phase [1].
In vitro, CGP 53353 selectively inhibits PKCβII with an IC50 of 0.41 μM, compared to 3.8 μM for PKCβI. It inhibits prionogenic Sup35 fibrillization with an IC50 of approximately 3.4 μM and inhibits the de novo assembly of Aβ42. The compound demonstrates potent and selective inhibition of PKCβII. |
| ln Vivo |
In vivo, CGP 53353 has been studied for its effects on PKCβII-mediated signaling pathways. As a selective PKCβII inhibitor, it may modulate cellular processes involved in cancer, inflammation, and neurodegenerative diseases. Specific in vivo data including efficacy in disease models are available from published studies.
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| Enzyme Assay |
In vitro kinase assays for PKCβII inhibition typically use recombinant PKCβII enzyme and a suitable peptide substrate. The enzyme is incubated with ATP, lipid activators (e.g., phosphatidylserine, diacylglycerol), and the substrate in the presence of varying concentrations of CGP 53353. Kinase activity is measured by detecting phosphorylation of the substrate using radiometric or luminescence-based methods. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell proliferation assay
Cell Types: A10 (glucose-induced cell proliferation) [1] Tested Concentrations: 1 μM Incubation Duration: 48-96 hrs (hours) Experimental Results: Although increasing glucose concentration stimulated A10 cell proliferation, it inhibited glucose-induced cell proliferation. In vitro cellular assays for PKC inhibitors typically use cancer cell lines or cells expressing PKCβII. Cells are treated with CGP 53353 at various concentrations, and PKCβII-mediated phosphorylation of downstream targets is assessed by Western blotting. Cell proliferation is measured by MTT or CCK-8 assays. Apoptosis is assessed by Annexin V/PI staining. |
| Animal Protocol |
In vivo animal studies for PKC inhibitors typically use xenograft tumor models or models of inflammatory diseases. Animals are administered CGP 53353 via various routes, and disease progression is monitored. PKCβII target engagement and pathway modulation are assessed in tissue samples by Western blotting or immunohistochemistry.
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| ADME/Pharmacokinetics |
CGP 53353 is a small-molecule PKC inhibitor with physicochemical properties suitable for research use. It is soluble in DMSO (36.53 mg/mL). The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CGP 53353 would typically include acute and repeated-dose toxicity in rodents, as well as genotoxicity and safety pharmacology assessments. As a PKC inhibitor, potential effects on immune function and cardiovascular system should be monitored. The compound is generally well-tolerated at therapeutic doses.
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| References | |
| Additional Infomation |
5,6-Bis(4-fluoroaniline)isoindole-1,3-dione is a phthalimide compound.
CGP 53353 (DAPH-7) is a selective inhibitor of PKCβII with an IC50 of 0.41 μM, compared to 3.8 μM for PKCβI. It also inhibits Sup35 fibrillization and Aβ42 assembly. The compound is available for research use only and is not approved for clinical use. |
| Molecular Formula |
C20H13F2N3O2
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|---|---|
| Molecular Weight |
365.34
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| Exact Mass |
365.097
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| Elemental Analysis |
C, 65.75; H, 3.59; F, 10.40; N, 11.50; O, 8.76
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| CAS # |
145915-60-2
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| PubChem CID |
6711154
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.703
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| LogP |
3.89
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
511
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(NC2C=C3C(NC(=O)C3=CC=2NC2C=CC(F)=CC=2)=O)=CC=1
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| InChi Key |
RONQPWQYDRPRGG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13F2N3O2/c21-11-1-5-13(6-2-11)23-17-9-15-16(20(27)25-19(15)26)10-18(17)24-14-7-3-12(22)4-8-14/h1-10,23-24H,(H,25,26,27)
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| Chemical Name |
5,6-bis(4-fluoroanilino)isoindole-1,3-dione
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| Synonyms |
CGP-53353; CGP 53353; CGP53353
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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 (~136.86 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 | 2.7372 mL | 13.6859 mL | 27.3718 mL | |
| 5 mM | 0.5474 mL | 2.7372 mL | 5.4744 mL | |
| 10 mM | 0.2737 mL | 1.3686 mL | 2.7372 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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