| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
H7 dihydrochloride targets multiple serine/threonine protein kinases, including protein kinase A (PKA), protein kinase C (PKC), protein kinase G (PKG), and myosin light chain kinase (MLCK). It acts as an ATP-competitive inhibitor, binding to the ATP-binding site of these kinases and preventing their phosphorylation of downstream substrates. At 100 µM, H7 dihydrochloride completely inhibits both TPA (12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ornithine decarboxylase (ODC) activity. It also inhibits cell invasion and metastasis in B16BL6 cancer cells through the PKC/MEK/ERK pathway and inhibits Topo.
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| ln Vitro |
In vitro, H7 dihydrochloride demonstrates potent inhibition of multiple serine/threonine protein kinases with Ki values of 3.0 µM for PKA, 6.0 µM for PKC, 5.8 µM for PKG, and 97 µM for MLCK. At 100 µM, it completely inhibits TPA- and phospholipase C-induced ODC activity. It induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. H7 also inhibits telomerase activity in quercetin-, H-89-, or herbimycin A-treated NPC-076 cells. The compound inhibits cell invasion and metastasis in B16BL6 cancer cells through the PKC/MEK/ERK pathway.
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| ln Vivo |
Specific in vivo data for H7 dihydrochloride are not extensively detailed in the available literature. However, it has been used to study H-7-induced inhibition of contractility in rat embryo fibroblasts (REF52) cells. It blocks human immunodeficiency virus (HIV-1) replication in MOLT-4 cells. As a broad-spectrum kinase inhibitor, H7 dihydrochloride is primarily employed as a research tool in cell-based and biochemical assays to elucidate the role of protein kinases in various cellular processes.
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| Enzyme Assay |
The enzymatic activity of H7 dihydrochloride is assessed using cell-free kinase assays with recombinant or purified protein kinases. The kinase of interest (e.g., PKA, PKC, PKG, or MLCK) is incubated with a peptide substrate and ATP in the presence of varying concentrations of the inhibitor. The extent of phosphorylation is measured using radioactive labeling (e.g., ³²P-ATP) or fluorescence-based detection methods. The Ki or IC50 values for kinase inhibition are determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of H7 dihydrochloride, various cell lines can be used. Cells are treated with the compound at concentrations ranging from 1 to 100 µM for defined periods. Cell viability, proliferation, and apoptosis are assessed using standard assays such as MTT, trypan blue exclusion, or Annexin V/PI staining. The inhibition of specific kinase activities in cells is confirmed by Western blotting using phospho-specific antibodies against known kinase substrates.
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| Animal Protocol |
In vivo studies with H7 dihydrochloride typically involve administration to animal models via intraperitoneal or intravenous injection. The compound's effects on disease progression, such as tumor growth or viral replication, are monitored. Pharmacodynamic markers, including the phosphorylation status of kinase substrates in target tissues, are measured to confirm target engagement. However, detailed in vivo protocols for H7 are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
H7 dihydrochloride has a molecular formula of C₁₄H₁₇N₃O₂S·2HCl and a molecular weight of 352.28 g/mol. It is a light yellow lyophilized solid with a solubility of 20 mg/mL in water. The compound should be stored at 2-8°C, protected from light. Aqueous stock solutions are stable for up to 6 months at 4°C. It is soluble in water and DMSO.
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| Toxicity/Toxicokinetics |
H7 dihydrochloride is classified as a standard handling toxicity compound (Toxicity: Standard Handling A). As with all research chemicals, appropriate safety precautions should be taken during handling, including the use of personal protective equipment. Specific LD50 values and detailed toxicological profiles are not provided in the available literature.
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| References | |
| Additional Infomation |
1-(5-Isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride is a hydrochloride prepared from phenethylidine and two molar equivalents of hydrogen chloride. It is an EC 2.7.11.13 (protein kinase C) inhibitor. It contains 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (2+).
H7 dihydrochloride (also known as Protein Kinase Inhibitor H-7) is a broad-based, cell-permeable, reversible, ATP-competitive serine/threonine kinase inhibitor. It is an isoquinolinesulfonamide derivative widely used as a research tool to study kinase-mediated signaling pathways. H7 dihydrochloride is not a clinically approved drug but is extensively employed in biochemical and pharmacological research to investigate the roles of PKA, PKC, PKG, and MLCK in various cellular processes including apoptosis, cell cycle regulation, and cancer metastasis. |
| Molecular Formula |
C14H17N3O2S.2[HCL]
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|---|---|
| Molecular Weight |
364.29056
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| Exact Mass |
363.057
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| CAS # |
108930-17-2
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| Related CAS # |
Protein kinase inhibitor H-7;84477-87-2
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| PubChem CID |
73332
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| Appearance |
White to off-white solid powder
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| Boiling Point |
495.3ºC at 760mmHg
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| Melting Point |
215-225 °C
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| Flash Point |
253.3ºC
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| Vapour Pressure |
6E-10mmHg at 25°C
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| LogP |
4.168
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
434
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OARGPFMFRLLKPF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N3O2S.2ClH/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;2*1H
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| Chemical Name |
5-(2-methylpiperazin-1-yl)sulfonylisoquinoline;dihydrochloride
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~16.67 mg/mL (~45.76 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 | 2.7451 mL | 13.7253 mL | 27.4507 mL | |
| 5 mM | 0.5490 mL | 2.7451 mL | 5.4901 mL | |
| 10 mM | 0.2745 mL | 1.3725 mL | 2.7451 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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