| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
HA-100 targets multiple serine/threonine protein kinases. Its primary targets include cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and myosin light chain kinase (MLC-kinase). The IC₅₀ values are 4 μM for PKG, 8 μM for PKA, 12 μM for PKC, and 240 μM for MLC-kinase. The Kᵢ values for PKC and MLC-kinase are 6.5 μM and 61 μM, respectively. HA-100 also exhibits ROCK inhibitory activity.
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| ln Vitro |
HA-100 exerts a compensating inhibitory effect with Kis of 6.5 μM and 61 μM on ATP of PKC and mlc-cleavage, respectively [1].
In vitro, HA-100 acts as a competitive inhibitor with respect to ATP for PKC and MLC-kinase. It demonstrates broad-spectrum inhibitory activity against several key serine/threonine kinases. The compound's inhibitory effects have been quantified in both biochemical and cellular assays. HA-100 is used to study the role of these kinases in various cellular processes, including signal transduction, cell proliferation, and differentiation. |
| ln Vivo |
In vivo, HA-100 is employed in model systems to investigate kinase signaling pathways. It has been studied for its effects on cancer development, as it inhibits methyl glycosides implicated in tumor progression. The compound's cell-permeable nature allows it to be used in various in vivo experimental settings. However, specific in vivo efficacy data and detailed animal model studies are less extensively documented compared to its in vitro characterization.
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| Enzyme Assay |
Cell-free enzyme assays for HA-100 typically involve in vitro kinase inhibition assays using purified target kinases. The general protocol involves preparing a reaction mixture in a 96-well plate containing kinase assay buffer, the target kinase, a specific substrate, and various concentrations of HA-100. ATP is added to initiate the reaction. After incubation, the amount of phosphorylated substrate is measured using techniques such as radioactivity (³³P-ATP incorporation), fluorescence, or luminescence. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for HA-100 involve treating cultured cells with the compound to assess its effects on kinase-mediated signaling pathways. Cells are seeded in appropriate culture plates and allowed to adhere. HA-100 is then added at various concentrations and incubated for a designated period. Cellular effects are evaluated by measuring downstream signaling events, such as protein phosphorylation levels via Western blot, cell proliferation, or other phenotypic changes. The compound's high purity supports reproducible assay results.
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| Animal Protocol |
In vivo animal studies with HA-100 typically involve administration of the compound to animal models to investigate its effects on kinase-related pathways. The compound is often dissolved in suitable vehicles and administered via intraperitoneal, oral, or intravenous routes. Dosing regimens and treatment durations vary depending on the specific experimental model. Endpoints may include tissue analysis for kinase activity, biomarker measurement, and assessment of physiological or behavioral changes.
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| ADME/Pharmacokinetics |
HA-100 dihydrochloride is soluble in DMSO (up to ~150 mg/mL) and has good solubility in aqueous buffers. It is stable as a powder at -20°C for up to 3 years and in solution at -80°C for 6 months. For in vivo studies, it can be formulated in various vehicles to achieve the desired concentration. The compound has a molecular weight of 277.34 and a LogP of 2.176. It is stable at room temperature for short periods during shipping.
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| References | |
| Additional Infomation |
5-(1-piperazinylsulfonyl)isoquinoline is a member of the isoquinoline class of compounds.
The dihydrochloride salt form is used for enhanced stability and solubility. HA-100 is structurally related to other isoquinolinesulfonamide protein kinase inhibitors such as H-7, H-8, and H-9, but with a distinct selectivity profile. The compound is also known as C-1 and is used in stem cell research applications. It is supplied as a solid suitable for biochemical and cell-based kinase assays. HA-100 is for research use only and not for human therapeutic use. |
| Molecular Formula |
C13H15N3O2S
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|---|---|
| Molecular Weight |
277.34200
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| Exact Mass |
277.088
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| CAS # |
84468-24-6
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| Related CAS # |
HA-100 hydrochloride;141543-63-7;HA-100 dihydrochloride;210297-47-5
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| PubChem CID |
3545
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| Appearance |
White to off-white solid powder
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| Density |
1.332g/cm3
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| Boiling Point |
497.4ºC at 760 mmHg
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| Flash Point |
254.6ºC
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| Index of Refraction |
1.639
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| LogP |
2.176
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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 |
19
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UPTYCYWTFGTCCG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H15N3O2S/c17-19(18,16-8-6-14-7-9-16)13-3-1-2-11-10-15-5-4-12(11)13/h1-5,10,14H,6-9H2
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| Chemical Name |
5-piperazin-1-ylsulfonylisoquinoline
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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) |
DMSO : ~150 mg/mL (~540.85 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6057 mL | 18.0284 mL | 36.0568 mL | |
| 5 mM | 0.7211 mL | 3.6057 mL | 7.2114 mL | |
| 10 mM | 0.3606 mL | 1.8028 mL | 3.6057 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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