| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ROCK1 (Rho-associated protein kinase 1), also known as Rho-associated coiled-coil containing protein kinase 1. GSK299115A is a selective ROCK1 inhibitor with an IC50 of 8 nM. It also inhibits RSK1 with an IC50 of 620 nM and p70S6K with an IC50 of 560 nM. Additionally, GSK299115A is a G protein-coupled receptor kinase (GRK) and PKA inhibitor. GRK2 is ubiquitously expressed in many tissues and regulates various intracellular mechanisms.
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| ln Vitro |
GSK299115A inhibits ROCK1 with an IC50 of 8 nM. It also inhibits RSK1 (IC50 = 620 nM) and p70S6K (IC50 = 560 nM). As a GRK and PKA inhibitor, it modulates G protein-coupled receptor signaling and protein kinase A pathways. The compound's selectivity profile makes it a valuable tool for studying ROCK1 and GRK2 function in various cellular contexts.
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| ln Vivo |
Specific in vivo activity data for GSK299115A are not extensively reported in the available literature. As a ROCK1 and GRK2 inhibitor, it could have effects on cardiovascular function, smooth muscle contraction, and neuronal signaling. ROCK1 inhibitors have been investigated for their potential in treating hypertension, glaucoma, and other conditions. Specific animal model studies are not described in the available sources.
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| Enzyme Assay |
In vitro kinase inhibition assays for GSK299115A involve measuring the activity of ROCK1, RSK1, p70S6K, GRK, or PKA in the presence of varying concentrations of the compound. The enzyme is incubated with ATP and a substrate peptide, and the phosphorylation of the substrate is quantified. The IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for GSK299115A assess its effects on ROCK1- or GRK2-dependent signaling in cells. Cells are treated with GSK299115A, and the phosphorylation of downstream targets is measured by Western blotting or ELISA. The compound's effects on cell morphology, migration, or other functional endpoints can also be evaluated. The compound is soluble in DMSO at 50 mg/mL.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK299115A are not described in the available literature. To evaluate its in vivo activity, GSK299115A could be administered to animal models of cardiovascular or neurological diseases where ROCK1 or GRK2 plays a role. Endpoints would depend on the specific disease model being studied.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK299115A are not reported in the available literature. As a small molecule inhibitor with a molecular weight of 415.27, it is expected to have reasonable absorption properties. The compound is typically stored as a powder at -20°C for long-term stability and is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK299115A are not available in the searched literature. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
GSK299115A is a research tool for studying ROCK1, GRK, and PKA function. GRK2 has been implicated in the progression of heart failure, and the compound may be useful as a chemical probe for therapeutic applications ranging from heart failure to neurological disorders. It is not an approved therapeutic agent.
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| Molecular Formula |
C20H16CL2N4O2
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|---|---|
| Molecular Weight |
415.28
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| Exact Mass |
414.065
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| CAS # |
864082-35-9
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| PubChem CID |
11247002
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
671
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(CC(=O)N1)C2=CC(=C(C=C2)Cl)Cl)C(=O)NC3=CC4=C(C=C3)NN=C4
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| InChi Key |
RHTXWIKPNGROHZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16Cl2N4O2/c1-10-19(20(28)25-13-3-5-17-12(6-13)9-23-26-17)14(8-18(27)24-10)11-2-4-15(21)16(22)7-11/h2-7,9,14H,8H2,1H3,(H,23,26)(H,24,27)(H,25,28)
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| Chemical Name |
4-(3,4-dichlorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyridine-5-carboxamide
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| Synonyms |
GSK-299115A; GSK 299115A; GSK299115A
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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 | 2.4080 mL | 12.0401 mL | 24.0801 mL | |
| 5 mM | 0.4816 mL | 2.4080 mL | 4.8160 mL | |
| 10 mM | 0.2408 mL | 1.2040 mL | 2.4080 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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