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| Targets |
Prostratin targets protein kinase C (PKC), a family of serine/threonine kinases that play a critical role in various cellular processes, including cell proliferation, differentiation, and apoptosis. It is a PKC activator with a Ki of 12.5 nM. Prostratin is also an NF-κB activator. By activating PKC and NF-κB, Prostratin modulates gene expression and cellular signaling pathways.
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| ln Vitro |
Prostratin has a Ki of 210 nM and transcribes [3H]PDBu binding to CEM cells [1]. Transcriptional acute myeloid leukemia (AML) cell lines (HL-60, NB4, and U937 cells) are not able to proliferate at concentrations of prostratin (125-1000 nM). In HL-60 cells, prostatretin (125–100 nM) influences cell cycle-related molecules (pRb phosphorylation, CDK, and p21) and causes G1 arrest in AML cells. Prostratin also activates PKC, which causes AML cell lines to become active. Moreover, humidity produced by prostaglandin is necessary for PKC-driven activation of MEK/ERK/MAP signal load [2]. For HIV-1-induced activation, prostatin induction necessitates the active form of PKD3. Moreover, prostratein activates PKD3 via PKCε of the new PKC subfamily [2].
In vitro, Prostratin is an activator of PKC with a Ki of 12.5 nM. It activates the NF-κB pathway. Prostratin has been shown to inhibit the activity of HIV-1. Its activity is typically measured using kinase assays and cell-based reporter assays. These in vitro studies confirm Prostratin's activity as a PKC and NF-κB activator. |
| ln Vivo |
In vivo, Prostratin is an orally active compound. As a PKC and NF-κB activator, it has potential applications in the study of HIV latency, cancer, and other diseases. However, specific in vivo protocols and results are not detailed in standard product descriptions.
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| Enzyme Assay |
In vitro kinase assays for Prostratin measure its activation of PKC. PKC is incubated with a peptide substrate and ATP in the presence of varying concentrations of Prostratin. The incorporation of phosphate into the substrate is measured, and the EC50 is determined. NF-κB activation can be measured using reporter gene assays.
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| Cell Assay |
Cell viability assay [2]
Cell Types: HL-60, NB4 and U937 Cell Tested Concentrations: 125nM, 250nM, 500nM, 1000nM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: dose-dependent inhibition 3]. Growth of acute myeloid leukemia (AML) cell lines. Cell cycle analysis[2] Cell Types: HL-60, NB4 and U937 Cell Tested Concentrations: 125 nM, 250 nM, 500 nM, 1000 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induced G0/G1 phase accumulation in a concentration-dependent manner. Western Blot Analysis[2] Cell Types: HL-60 Cell Tested Concentrations: 125 nM, 250 nM, 500 nM, 1000 nM Incubation Duration: 24 hrs (hours) Experimental Results: Effects of cell cycle related molecules (pRb phosphorylation, CDK and p21) in HL- in 60 cells. In vitro cell-based assays for Prostratin are used to study its effects on PKC and NF-κB signaling. Cells are treated with Prostratin, and the activation of PKC and NF-κB is measured. The compound's ability to inhibit HIV-1 replication can also be assessed in cell-based assays. |
| Animal Protocol |
In vivo animal experiments for Prostratin are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a PKC activator would involve its administration to animal models of cancer or HIV infection. However, specific protocols for Prostratin are not detailed.
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| ADME/Pharmacokinetics |
Prostratin has a molecular weight of 390.47 g/mol and a molecular formula of C22H30O6. It has a CAS number of 60857-08-1. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. Prostratin is orally active.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Prostratin is not provided in standard product descriptions. As a PKC activator, it may have significant biological effects and potential toxicity. As with all research chemicals, standard laboratory safety precautions should be followed when handling Prostratin. Its use is limited to research applications.
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| References |
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| Additional Infomation |
Prostratin are phorbol esters that function as a metabolite. They have been reported to be found in Euphorbia trifoliata, Euphorbia fischeriana, and other organisms with relevant data.
Prostratin is a research compound and is not approved for any clinical or therapeutic use. It is a naturally occurring diterpenoid that is an activator of protein kinase C (PKC) with a Ki of 12.5 nM. It is also an NF-κB activator. Prostratin has been shown to inhibit the activity of HIV-1. It is a valuable research tool for studying PKC signaling, HIV latency, and cancer. |
| Molecular Formula |
C22H30O6
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| Molecular Weight |
390.4700
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| Exact Mass |
390.204
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| CAS # |
60857-08-1
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| PubChem CID |
454217
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
550.5±50.0 °C at 760 mmHg
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| Melting Point |
216-219℃
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| Flash Point |
188.7±23.6 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
1.84
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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 |
3
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| Heavy Atom Count |
28
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| Complexity |
825
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@H]1C[C@@]2([C@@H](C2(C)C)[C@H]3[C@]1([C@@H]4C=C(C(=O)[C@]4(CC(=C3)CO)O)C)O)OC(=O)C
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| InChi Key |
BOJKFRKNLSCGHY-HXGSDTCMSA-N
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| InChi Code |
InChI=1S/C22H30O6/c1-11-6-16-20(26,18(11)25)9-14(10-23)7-15-17-19(4,5)21(17,28-13(3)24)8-12(2)22(15,16)27/h6-7,12,15-17,23,26-27H,8-10H2,1-5H3/t12-,15+,16-,17-,20-,21+,22-/m1/s1
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| Chemical Name |
[(1R,2S,6R,10S,11R,13S,15R)-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-13-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] acetate
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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 : ~50 mg/mL (~128.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5610 mL | 12.8051 mL | 25.6102 mL | |
| 5 mM | 0.5122 mL | 2.5610 mL | 5.1220 mL | |
| 10 mM | 0.2561 mL | 1.2805 mL | 2.5610 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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