| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Protein Kinase C 19-36 targets protein kinase C (PKC) isoforms by acting as a pseudosubstrate inhibitor. PKC is a family of serine/threonine kinases that play critical roles in cell signaling, regulating diverse cellular processes including proliferation, differentiation, apoptosis, and gene expression. PKC isoforms are activated by diacylglycerol (DAG) and calcium (for conventional isoforms) or by DAG alone (for novel isoforms). 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 19-36 is a synthetic peptide that corresponds to this pseudosubstrate sequence, competitively inhibiting PKC by blocking substrate access to the catalytic site. The peptide inhibits PKC with an IC₅0 of 0.18 microM.
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| ln Vitro |
In vitro, Protein Kinase C 19-36 inhibits PKC with an IC₅0 of 0.18 microM (180 nM). The peptide effectively slows down vascular proliferation and hypertrophy. It also inhibits glucose-induced natriuretic peptide receptor response. The pseudosubstrate peptide is a highly specific inhibitor of PKC, as it mimics the endogenous autoinhibitory sequence and does not interfere with other kinases. The peptide is used in research to investigate the role of PKC in various cellular processes including signal transduction, cell cycle regulation, and disease pathogenesis. The high potency and specificity of Protein Kinase C 19-36 make it a valuable tool for studying PKC-mediated signaling pathways.
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| ln Vivo |
In vivo data for Protein Kinase C 19-36 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 and in vivo studies to demonstrate the role of PKC in vascular proliferation and hypertrophy. The peptide inhibits glucose-induced natriuretic peptide receptor responses, suggesting a role for PKC in this pathway. The compound is intended for research use only and is not for human therapeutic applications.
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| Enzyme Assay |
In vitro enzyme assays for Protein Kinase C 19-36 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., a PKC substrate peptide such as histone H1 or a specific 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 19-36 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. Vascular hypertrophy is assessed by measuring cell size or protein content. 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 19-36 are limited but have been conducted in models of vascular disease. In typical 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, due to the peptide's limited bioavailability, such studies are challenging. Researchers should consult the primary literature for the most current information.
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| ADME/Pharmacokinetics |
Protein Kinase C 19-36 (CAS#: 113731-96-7) has molecular formula C₉3H1₅₉N3₅O24 and molecular weight 2151.48. The peptide sequence corresponds to residues 19-36 of the PKC pseudosubstrate domain. It is a pseudosubstrate peptide inhibitor of protein kinase C (PKC) with an IC₅0 of 0.18 microM. The peptide is used in research to study PKC-mediated signaling pathways. It is supplied for research use only and is not for human therapeutic applications. The peptide should be stored at -20degC and is soluble in water or DMSO. The peptide is typically purified to >95% purity.
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| Toxicity/Toxicokinetics |
Toxicological information for Protein Kinase C 19-36 is limited as the compound is a research peptide. As a pseudosubstrate peptide, it specifically inhibits PKC and may have effects on PKC-dependent cellular processes. The peptide should be handled with standard laboratory precautions including the use of personal protective equipment. Avoid inhalation, ingestion, and skin contact. The peptide should be stored at -20degC and disposed of according to institutional guidelines for biological and chemical waste.
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| References | |
| Additional Infomation |
Protein Kinase C 19-36 (CAS#: 113731-96-7) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), corresponding to residues 19-36 of the PKC pseudosubstrate domain. The peptide inhibits PKC with an IC₅0 of 0.18 microM. Pseudosubstrate peptides are widely used as research tools to study the role of PKC in various cellular processes including signal transduction, cell proliferation, differentiation, and apoptosis. Protein Kinase C 19-36 effectively slows down vascular proliferation and hypertrophy and inhibits glucose-induced natriuretic peptide receptor response. The peptide is supplied for research use only and is not approved for clinical use. As of the current date, Protein Kinase C 19-36 remains a preclinical research tool.
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| Molecular Formula |
C93H159N35O24
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| Molecular Weight |
2151.4777
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| Exact Mass |
2150.23
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| CAS # |
113731-96-7
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| PubChem CID |
71308428
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| Appearance |
White to off-white solid powder
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| LogP |
4.055
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| Hydrogen Bond Donor Count |
36
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| Hydrogen Bond Acceptor Count |
32
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| Rotatable Bond Count |
80
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| Heavy Atom Count |
152
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| Complexity |
4570
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| Defined Atom Stereocenter Count |
17
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=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)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CCCNC(=N)N)N
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| InChi Key |
NHCJMYZDRROLEW-OFXZVSIYSA-N
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| InChi Code |
InChI=1S/C93H159N35O24/c1-47(2)39-62(122-74(135)50(7)113-70(132)45-111-77(138)55(24-12-15-33-94)116-78(139)58(27-19-37-109-92(103)104)115-75(136)51(8)114-84(145)63(40-52-21-10-9-11-22-52)123-76(137)54(97)23-18-36-108-91(101)102)85(146)118-59(28-20-38-110-93(105)106)79(140)119-60(29-31-67(98)129)82(143)117-56(25-13-16-34-95)80(141)124-65(42-68(99)130)87(148)128-73(49(5)6)89(150)125-64(41-53-44-107-46-112-53)86(147)120-61(30-32-71(133)134)83(144)127-72(48(3)4)88(149)121-57(26-14-17-35-96)81(142)126-66(90(151)152)43-69(100)131/h9-11,21-22,44,46-51,54-66,72-73H,12-20,23-43,45,94-97H2,1-8H3,(H2,98,129)(H2,99,130)(H2,100,131)(H,107,112)(H,111,138)(H,113,132)(H,114,145)(H,115,136)(H,116,139)(H,117,143)(H,118,146)(H,119,140)(H,120,147)(H,121,149)(H,122,135)(H,123,137)(H,124,141)(H,125,150)(H,126,142)(H,127,144)(H,128,148)(H,133,134)(H,151,152)(H4,101,102,108)(H4,103,104,109)(H4,105,106,110)/t50-,51-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,72-,73-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]acetyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-5-[[(2S)-1-[[(2S)-6-amino-1-[[(1S)-3-amino-1-carboxy-3-oxopropyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic 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) |
H2O : ~100 mg/mL (~46.48 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (4.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4648 mL | 2.3240 mL | 4.6480 mL | |
| 5 mM | 0.0930 mL | 0.4648 mL | 0.9296 mL | |
| 10 mM | 0.0465 mL | 0.2324 mL | 0.4648 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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