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| Targets |
Protein Kinase C 19-31 targets protein kinase C (PKC) isoforms by acting as a pseudosubstrate inhibitor. The pseudosubstrate domain of PKC is a conserved autoinhibitory region that keeps the kinase in an inactive state by occupying the substrate-binding site. Protein Kinase C 19-31 is a synthetic peptide that corresponds to this pseudosubstrate sequence, competitively inhibiting PKC by blocking substrate access to the catalytic site. The peptide is derived from the pseudosubstrate regulatory domain of PKCalpha (residues 19-31). PKC is a potential target for the development of drugs for the treatment of cancer, diabetes, and other diseases.
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| ln Vitro |
In vitro, Protein Kinase C 19-31 inhibits PKC activity by acting as a pseudosubstrate inhibitor. The peptide competitively binds to the substrate-binding site of PKC, blocking access to physiological substrates and preventing phosphorylation. The peptide sequence is RFARKGALRQKNV, which corresponds to the pseudosubstrate domain of PKCalpha. In cellular assays, the peptide inhibits PKC-mediated signaling pathways, including phosphorylation of downstream substrates. The peptide is used in research to investigate the role of PKC in various cellular processes including cell proliferation, differentiation, apoptosis, and gene expression. PKC is a potential target for drug development in cancer, diabetes, and other diseases.
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| ln Vivo |
In vivo data for Protein Kinase C 19-31 are limited as the peptide is primarily used as a research tool in in vitro experiments. Peptide inhibitors generally have limited in vivo utility due to poor stability, low bioavailability, and rapid clearance. However, the peptide has been used in some ex vivo studies to demonstrate the role of PKC in various signaling pathways. The compound is intended for research use only and is not for human therapeutic applications. Researchers interested in in vivo applications should consult the primary literature for the most current information.
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| Enzyme Assay |
In vitro enzyme assays for Protein Kinase C 19-31 involve measuring PKC activity using recombinant PKC isoforms or PKC isolated from tissue extracts. The assay is performed in kinase buffer containing ATP, Mg2+, phosphatidylserine, and diacylglycerol (for activation) with a peptide substrate (e.g., histone H1 or a specific PKC substrate peptide). Varying concentrations of the pseudosubstrate peptide (0.001-10 microM) are pre-incubated with the enzyme before adding the substrate and ATP. After incubation at 30degC for 10-30 minutes, kinase activity is quantified by measuring incorporation of [33P]-ATP into the substrate or by using a fluorescence-based or luminescence-based detection system (ADP-Glo). IC₅0 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Protein Kinase C 19-31 are performed using various cell lines to study PKC-dependent signaling pathways. Cells (e.g., vascular smooth muscle cells, endothelial cells, or cancer cells) are cultured in appropriate medium and seeded in 6- or 96-well plates. The peptide is delivered into cells using cell-penetrating peptide sequences or lipofection due to its limited cell permeability. Cells are treated with the peptide (0.1-10 microM) for 1-24 hours. PKC activity is assessed by Western blotting for phosphorylation of PKC substrates (e.g., MARCKS, GAP-43). Cell proliferation is measured by [3H]-thymidine incorporation or BrdU labeling. Apoptosis is assessed by caspase-3/7 activity and Annexin V staining. Signaling pathway activation is evaluated by Western blotting for downstream effectors.
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| Animal Protocol |
In vivo animal studies for Protein Kinase C 19-31 are limited due to the peptide's poor bioavailability and stability. In some studies, the peptide may be administered via local injection or using osmotic minipumps. For vascular studies, rats or mice are used to assess neointimal hyperplasia following vascular injury. The peptide is delivered locally to the injured vessel, and vascular remodeling is assessed by histomorphometry. In metabolic studies, the peptide is used to investigate the role of PKC in glucose-induced signaling. However, specific protocols and dosing regimens have not been well-established. Researchers should consult the primary literature for the most current information.
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| ADME/Pharmacokinetics |
Protein Kinase C 19-31 (CAS#: 121545-65-1) has molecular formula C₆₇H11₈N2₆O1₆ and molecular weight 1,543.82. The peptide sequence is RFARKGALRQKNV. It is a pseudosubstrate peptide inhibitor of protein kinase C (PKC) derived from the pseudosubstrate regulatory domain of PKCalpha (residues 19-31). The compound is a research chemical for laboratory use only. It is not for human therapeutic applications. The peptide should be stored at -20degC and is soluble in water or DMSO. Purity is typically >95%.
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| References | |
| Additional Infomation |
Protein Kinase C 19-31 (CAS#: 121545-65-1), also known as PKC (19-31), is a pseudosubstrate peptide inhibitor of protein kinase C (PKC) derived from the pseudosubstrate regulatory domain of PKCalpha (residues 19-31). PKC is a family of serine/threonine kinases involved in controlling cell proliferation, differentiation, apoptosis, and gene expression through the phosphorylation of serine and threonine residues on target proteins. PKC is a potential target for drug development in cancer, diabetes, and other diseases. The peptide is used as a research tool to study PKC-mediated signaling pathways. As of the current date, Protein Kinase C 19-31 is not approved for clinical use.
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| Molecular Formula |
C67H118N26O16
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|---|---|
| Molecular Weight |
1543.82000
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| Exact Mass |
1542.92
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| CAS # |
121545-65-1
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| Related CAS # |
Protein Kinase C (19-31) (TFA)
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| PubChem CID |
25084468
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| Appearance |
White to off-white solid powder
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| LogP |
3.785
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| Hydrogen Bond Donor Count |
24
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
55
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| Heavy Atom Count |
109
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| Complexity |
3080
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCN=C(N)N)N
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| InChi Key |
OLYXRRDLXDCSNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C67H118N26O16/c1-35(2)31-46(62(106)88-44(23-16-30-81-67(77)78)58(102)89-45(24-25-49(71)94)60(104)87-42(21-11-13-27-69)59(103)92-48(33-50(72)95)63(107)93-52(36(3)4)64(108)109)90-53(97)37(5)83-51(96)34-82-56(100)41(20-10-12-26-68)86-57(101)43(22-15-29-80-66(75)76)85-54(98)38(6)84-61(105)47(32-39-17-8-7-9-18-39)91-55(99)40(70)19-14-28-79-65(73)74/h7-9,17-18,35-38,40-48,52H,10-16,19-34,68-70H2,1-6H3,(H2,71,94)(H2,72,95)(H,82,100)(H,83,96)(H,84,105)(H,85,98)(H,86,101)(H,87,104)(H,88,106)(H,89,102)(H,90,97)(H,91,99)(H,92,103)(H,93,107)(H,108,109)(H4,73,74,79)(H4,75,76,80)(H4,77,78,81)
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| Chemical Name |
2-[[4-amino-2-[[6-amino-2-[[5-amino-2-[[2-[[2-[2-[[2-[[6-amino-2-[[2-[2-[[2-[[2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoyl]amino]propanoylamino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]acetyl]amino]propanoylamino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoic acid
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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) |
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 | 0.6477 mL | 3.2387 mL | 6.4774 mL | |
| 5 mM | 0.1295 mL | 0.6477 mL | 1.2955 mL | |
| 10 mM | 0.0648 mL | 0.3239 mL | 0.6477 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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