| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
0.9 μM (mycobacterial protein kinase G)[1]
The primary target of protein kinase G inhibitor-1 is mycobacterial protein kinase G (PKG). The compound inhibits PKG with an IC₅₀ value of 0.9 μM. Protein kinase G inhibitor-1 is a selective inhibitor targeting PKG. By inhibiting this kinase, the compound disrupts mycobacterial signaling pathways. The compound may be utilized to study mycobacterial infections. |
|---|---|
| ln Vitro |
In vitro studies have demonstrated that protein kinase G inhibitor-1 is a potent inhibitor of mycobacterial PKG with an IC₅₀ of 0.9 μM. The compound shows selective inhibition of PKG. Protein kinase G inhibitor-1 has been characterized as a potent inhibitor in biochemical assays. Its in vitro activity supports its use as a research tool for studying mycobacterial signaling.
|
| ln Vivo |
In vivo activity of protein kinase G inhibitor-1 has not been extensively reported. The compound is primarily used as a research tool for in vitro studies of PKG inhibition. Animal model studies evaluating its in vivo efficacy have not been published. Further investigations are needed to assess its therapeutic potential against mycobacterial infections.
|
| Enzyme Assay |
For PKG inhibition assays, recombinant mycobacterial protein kinase G is incubated with a peptide substrate and ATP in the presence of protein kinase G inhibitor-1. Kinase activity is measured using radioactive (³³P-ATP) or fluorescence-based (TR-FRET) detection methods. IC₅₀ values are calculated from dose-response curves. Standard protocols for kinase inhibition assays are described in the literature.
|
| Cell Assay |
For in vitro cell-based studies, mycobacterial cells such as Mycobacterium tuberculosis are cultured in appropriate media and treated with serial dilutions of protein kinase G inhibitor-1. Cell viability and growth inhibition are assessed. The compound's effects on mycobacterial signaling pathways may be analyzed by Western blotting. Cytotoxicity against mammalian cells may be assessed in parallel.
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| Animal Protocol |
In vivo animal studies for protein kinase G inhibitor-1 have not been extensively reported. For similar kinase inhibitors targeting mycobacteria, mouse models of tuberculosis infection may be used. The compound would be administered via oral or intraperitoneal routes. Efficacy endpoints include reduction in bacterial burden and survival. Standard protocols for in vivo efficacy studies can be adapted from the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of protein kinase G inhibitor-1 have not been comprehensively characterized. As a small molecule with a molecular weight of 278.37 g/mol, it is expected to have reasonable membrane permeability. The compound is soluble in DMSO at ≥100 mg/mL. Specific PK parameters such as half-life, clearance, and bioavailability have not been reported. Further pharmacokinetic studies are needed.
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| Toxicity/Toxicokinetics |
Toxicological data for protein kinase G inhibitor-1 are limited. As a research compound, standard toxicological studies have not been extensively published. Cytotoxicity against mammalian cell lines may be assessed in parallel with activity studies. The compound is for research use only and is not intended for human therapeutic use. Standard safety assessments would be needed for therapeutic development.
|
| References | |
| Additional Infomation |
Protein kinase G inhibitor-1 is a research compound for studying mycobacterial protein kinase G inhibition. It is also known as Compound 270 or WAY-312157. The compound may be utilized to study mycobacterial infections. No clinical trials or regulatory approvals have been reported for this compound. Protein kinase G inhibitor-1 serves as a research tool for studying kinase signaling and potential therapeutic strategies.
|
| Molecular Formula |
C14H18N2O2S
|
|---|---|
| Molecular Weight |
278.37
|
| Exact Mass |
278.108
|
| CAS # |
354544-70-0
|
| PubChem CID |
2862914
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
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| Boiling Point |
464.9±45.0 °C at 760 mmHg
|
| Flash Point |
234.9±28.7 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.660
|
| LogP |
2.97
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
19
|
| Complexity |
397
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1CCC2C(=C(SC=2C1)NC(C1CC1)=O)C(=O)N
|
| InChi Key |
PGBKHXTZZAKXMK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H18N2O2S/c1-7-2-5-9-10(6-7)19-14(11(9)12(15)17)16-13(18)8-3-4-8/h7-8H,2-6H2,1H3,(H2,15,17)(H,16,18)
|
| Chemical Name |
2-(cyclopropanecarbonylamino)-6-methyl-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
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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 | 3.5923 mL | 17.9617 mL | 35.9234 mL | |
| 5 mM | 0.7185 mL | 3.5923 mL | 7.1847 mL | |
| 10 mM | 0.3592 mL | 1.7962 mL | 3.5923 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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