| Size | Price | Stock | Qty |
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| 25mg |
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| Targets |
H-7 primarily targets Protein Kinase C (PKC) with a Ki of 6.0 μM, cAMP-dependent Protein Kinase (PKA) with an IC50 of 3.0 μM, and cGMP-dependent Protein Kinase (PKG) with an IC50 of 5.8 μM. It also inhibits myosin light chain kinase with an IC50 of 97.0 μM. Compared to its structural analog H-8, H-7 shows more potent inhibition of PKC (Ki 6.0 μM vs. 15.0 μM).
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| ln Vitro |
In vitro, H-7 blocks induction of ICAM-1 with IC50 values of 6-10 μM. It suppresses cell polarity of unstimulated control cells with an ID50 of 6.5 μM H-7. H-7 inhibits superoxide release from human neutrophils stimulated with phorbol myristate acetate or synthetic diacylglycerol. It blocks the induction of immediate-early genes zif268. H-7 has been widely used to characterize the functional roles of PKC in cellular processes.
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| ln Vivo |
In vivo, H-7 has been used in research models to study the role of protein kinases in various physiological and pathological processes. It has been investigated for its effects on cell polarity and locomotion in Walker 256 carcinosarcoma cells. The compound's ability to inhibit multiple serine/threonine kinases makes it valuable for studying kinase-dependent signaling pathways in vivo, though specific animal efficacy data is limited in the search results.
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| Enzyme Assay |
The in vitro activity of H-7 is assessed using cell-free kinase activity assays. For PKC inhibition, the enzyme is incubated with a substrate peptide (e.g., histone H1 or a synthetic peptide) and [γ-³²P]ATP in the presence of varying concentrations of H-7. The incorporation of radioactive phosphate into the substrate is measured, and the Ki or IC50 is calculated. For PKA and PKG assays, similar protocols are used with appropriate substrates and cofactors. IC50 values are determined from dose-response curves using nonlinear regression analysis.
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| Cell Assay |
For cellular assays, various cell lines are used depending on the pathway being studied. Human neutrophils are used to study superoxide release; cells are pre-incubated with H-7 (typically 1-100 μM) before stimulation with phorbol myristate acetate. ICAM-1 induction studies use endothelial cells treated with H-7 followed by cytokine stimulation, with ICAM-1 expression measured by flow cytometry or ELISA. Cell polarity studies use Walker 256 carcinosarcoma cells treated with H-7, with polarity assessed by microscopy.
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| Animal Protocol |
In vivo, H-7 is typically administered intraperitoneally or intravenously to animal models at doses ranging from 1-50 mg/kg. The compound is dissolved in suitable vehicles such as saline or DMSO. In tumor studies, H-7 is administered to mice bearing Walker 256 carcinosarcoma xenografts, and tumor growth, cell polarity, and locomotion are assessed. Tissue samples are collected for histological analysis and kinase activity measurement.
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| ADME/Pharmacokinetics |
H-7 has a molecular weight of 291.37 g/mol and a molecular formula of C14H17N3O2S. It is typically supplied as a dihydrochloride salt to enhance aqueous solubility for research applications. Solubility in ethanol is 20 mg/mL. The compound should be stored as powder at -20°C for up to 3 years or at 4°C for up to 2 years. It is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
Specific toxicity data for H-7 is not detailed in the provided search results. As a broad-spectrum kinase inhibitor, it may affect multiple cellular processes beyond its primary targets. The compound's IC50 values for various kinases range from 3.0 μM to 97 μM, suggesting a moderate safety window. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required for therapeutic applications.
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| References | |
| Additional Infomation |
5-(2-methylpiperazine-1-sulfonyl)isoquinoline belongs to the isoquinoline class and the N-sulfonylpiperazine class. It is an EC 2.7.11.13 (protein kinase C) inhibitor. It is a specific protein kinase C inhibitor that inhibits the release of superoxide from human neutrophils (PMNs) stimulated by phorbol myristate or synthetic diglycerides.
Protein kinase inhibitor H-7 is a well-established pharmacological tool for investigating signaling pathways dependent on PKC, PKA, and PKG. Its established inhibitory profile and frequent use in cellular assays have made it a standard reference compound. While other isoquinolinesulfonamides (e.g., H-8, HA-1004) and broad-spectrum inhibitors (e.g., Staurosporine) exist, they are not functionally interchangeable with H-7 for many applications. Each analog possesses a distinct inhibitory profile. H-7 is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C14H17N3O2S
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|---|---|
| Molecular Weight |
291.369
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| Exact Mass |
291.104
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| Elemental Analysis |
C, 57.71; H, 5.88; N, 14.42; O, 10.98; S, 11.00
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| CAS # |
84477-87-2
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| Related CAS # |
Protein kinase inhibitor H-7 dihydrochloride;108930-17-2
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| PubChem CID |
3542
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| Appearance |
White to light yellow solid powder
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| Density |
1.277 g/cm3
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| Boiling Point |
495.3ºC at 760 mmHg
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| Melting Point |
114 °C
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| Flash Point |
253.3ºC
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| Index of Refraction |
1.652
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| LogP |
2.564
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
434
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BDVFVCGFMNCYPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N3O2S/c1-11-9-16-7-8-17(11)20(18,19)14-4-2-3-12-10-15-6-5-13(12)14/h2-6,10-11,16H,7-9H2,1H3
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| Chemical Name |
5-(2-methylpiperazin-1-yl)sulfonylisoquinoline
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| Synonyms |
H-7 inhibitor; Protein kinase inhibitor H-7 ;
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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 : ~100 mg/mL (~343.21 mM)
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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 | 3.4321 mL | 17.1603 mL | 34.3206 mL | |
| 5 mM | 0.6864 mL | 3.4321 mL | 6.8641 mL | |
| 10 mM | 0.3432 mL | 1.7160 mL | 3.4321 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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