| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Rhodblock 6 targets the Rho kinase (ROCK) pathway. ROCK is a key regulator of the actin cytoskeleton and is involved in various cellular processes including contraction, motility, and proliferation. By inhibiting ROCK, it prevents the phosphorylation of MRLC.
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| ln Vitro |
ROCK activity is significantly inhibited in a dose-dependent manner by Rhodblock 6 (1-30 μM). Additionally, Rhodblock 6 inhibits its human homolog ROCK I. In human HeLa cells, Rhodblock 6 (100 μM; 20 hours) produces active fiber disruption [1].
In vitro, Rhodblock 6 acts as a ROCK inhibitor. Its activity is typically measured by assessing the phosphorylation levels of MRLC in cells treated with the compound. |
| ln Vivo |
Specific in vivo activity data for Rhodblock 6 is not detailed in the search results. Its effects are studied in cellular models to understand the role of ROCK in various biological processes.
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| Enzyme Assay |
The assay for ROCK activity involves a kinase assay using recombinant ROCK enzyme and a substrate. The reaction is carried out in the presence of ATP and varying concentrations of Rhodblock 6. The phosphorylation of the substrate is measured to determine the IC50 of the inhibitor.
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| Cell Assay |
Cells are treated with Rhodblock 6. The levels of phosphorylated MRLC (p-MRLC) are then measured, typically by Western blot using a phospho-specific antibody. The ability of the compound to inhibit MRLC phosphorylation is a direct readout of its cellular activity.
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| Animal Protocol |
In vivo studies for Rhodblock 6 are not described in the search results. As a research compound, it is primarily used in vitro and in cell-based assays.
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| ADME/Pharmacokinetics |
Rhodblock 6 has a molecular weight of 215.25 g/mol and a molecular formula of C12H13N3O. It is soluble in DMSO at ≥20 mg/mL.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Rhodblock 6 is not available in the search results. As a research chemical, standard safety precautions should be taken.
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| References | |
| Additional Infomation |
Rhodblock 6 is a research tool used to study the role of the Rho kinase (ROCK) pathway in cell biology. It is not a pharmaceutical drug.
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| Molecular Formula |
C12H13N3O
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|---|---|
| Molecular Weight |
215.25
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| Exact Mass |
215.106
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| CAS # |
886625-06-5
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| PubChem CID |
6466029
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| Appearance |
Pale purple to purple solid powder
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| LogP |
2.374
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
277
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GXJXOQKXBIPBKB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H13N3O/c16-12(8-2-1-3-8)14-10-4-5-11-9(6-10)7-13-15-11/h4-8H,1-3H2,(H,13,15)(H,14,16)
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| Chemical Name |
N-(1H-indazol-5-yl)cyclobutanecarboxamide
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| Synonyms |
Rhodblock6; Rhodblock-6; Rhodblock 6
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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 | 4.6458 mL | 23.2288 mL | 46.4576 mL | |
| 5 mM | 0.9292 mL | 4.6458 mL | 9.2915 mL | |
| 10 mM | 0.4646 mL | 2.3229 mL | 4.6458 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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