| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H22BrCl2N3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA), with an IC50 of 48 nM, and shows weak inhibition of PKG, PKC and Casein Kinase. It is supplied as a white to light yellow solid (C20H22BrCl2N3O2S, MW 519.28) at 99.97% purity.
Physical & Chemical Properties
| CAS Number | 130964-39-5 |
|---|---|
| Molecular Formula | C20H22BrCl2N3O2S |
| Molecular Weight | 519.28 g/mol |
| Purity | 99.97% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl |
| Signaling Pathway | Stem Cell/Wnt; TGF-beta/Smad; Autophagy |
| Solubility | In Vitro: DMSO: 100 mg/mL (192.57 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 5 mg/mL (9.63 mM; Requires sonication and warming and heat to 80°C) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 48 nM (protein kinase A)
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (192.57 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 5 mg/mL (9.63 mM) | requires sonication and warming and heat to 80°C |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% saline |
|---|---|
| Result | 5 mg/mL (9.63 mM); suspension; requires sonication |
Protocol 2
| Composition | 5% DMSO + 40% PEG300 + 5% Tween-80 + 50% saline |
|---|---|
| Result | ≥ 2.75 mg/mL (5.30 mM); clear solution |
Protocol 3
| Composition | 5% DMSO + 95% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.75 mg/mL (5.30 mM); clear solution |
Protocol 4
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.81 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 5
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (4.81 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 6
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.81 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Protocol 7
| Composition | 1% DMSO + 99% saline |
|---|---|
| Result | ≥ 0.55 mg/mL (1.06 mM); clear solution |
Data provided by the manufacturer.
In Vitro
H-89 inhibits protein kinase A in a manner competitive with ATP. H-89 dose-dependently inhibits forskolin-induced protein phosphorylation without lowering intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits forskolin-induced neurite outgrowth from PC12D cells. In PC12D cell lysates, H-89 (30 μM) significantly inhibits cAMP-dependent histone IIb phosphorylation activity[1]. In rat skinned fibers, H-89 (1-2 μM) significantly slows the repriming rate, most likely by adversely affecting the T-system potential. At 10-100 μM, H-89 inhibits net Ca2+ uptake by the SR and affects the Ca2+-sensitivity of the contractile apparatus in rat skinned fibers[2].
In Vivo
Seizure latency and threshold are significantly increased by H-89 (0.2 mg/100g, i.p.) in PTZ-treated animals. The epileptogenic activity of bucladesine (300 nM) is prevented by H-89 (0.05, 0.2 mg/100 g, i.p.), with a significant increase of seizure latency and seizure threshold[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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