| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C14H17N3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Protein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with Ki values of 6.0 μM against rabbit protein kinase C, 3.0 μM against rabbit cAMP-dependent protein kinase, and 5.8 μM against porcine cGMP-dependent protein kinase, while having no effect on Ca2+-calmodulin-dependent enzymes. It regulates the actin cytoskeleton: it inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid, reversible cytoskeletal reorganization[1][2][3]. It serves as a research tool for elucidating protein kinase C-mediated signaling systems, and it is supplied as a white to light yellow solid (C14H17N3O2S, MW 291.38) at 99.96% purity.
Physical & Chemical Properties
| CAS Number | 84477-87-2 |
|---|---|
| Molecular Formula | C14H17N3O2S |
| Molecular Weight | 291.38 g/mol |
| Purity | 99.96% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | O=S(C1=CC=CC2=C1C=CN=C2)(N3C(C)CNCC3)=O |
| Target | PKC, PKA, PKG |
| Signaling Pathway | Epigenetics; TGF-beta/Smad; Stem Cell/Wnt; Cytoskeleton |
| Solubility | In Vitro: DMSO: 100 mg/mL (343.19 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PKC 6 μM (Ki) |
PKA 3 μM (Ki) |
PKG 5.8 μM (Ki) |
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 (343.19 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
Protein kinase inhibitor H-7 acts as a potent, direct inhibitor of rabbit brain protein kinase C (Ki = 6.0 μM) as well as rabbit skeletal muscle cAMP-dependent protein kinase (Ki = 3.0 μM), while showing weak activity toward other purified protein kinases and ATPases from multiple species and tissues[1]. In intact washed rabbit platelets, protein kinase inhibitor H-7 (10-50 μM; 2 min preincubation) inhibits protein kinase C-mediated phosphorylation of the 40K protein in a dose-dependent manner, yet it does not inhibit Ca2+-calmodulin-mediated phosphorylation of the 20K protein in that same cellular system, even at 50 μM[2]. In Swiss 3T3 fibroblasts and SVT2 transformed fibroblasts, protein kinase inhibitor H-7 (100-300 μM) increases lamellipodial protrusive activity and lowers cell polarity, shown by a significant rise in dispersion value and a significant drop in elongation value[3]. In chicken lens cells, protein kinase inhibitor H-7 (300 μM; 10-30 min) breaks down stress fibers and focal adhesion-related proteins (myosin, vinculin, talin) but preserves intercellular adherens junctions; these cytoskeletal changes are fully reversible once H-7 is removed[3]. As a pretreatment, protein kinase inhibitor H-7 (300 μM; pretreatment for 10-15 min, or addition during permeabilization/contraction) strongly blocks ATP-induced contraction in Swiss 3T3 fibroblasts, chicken lens cells and chicken embryo fibroblasts permeabilized with Saponin, but inhibits contraction only weakly when it is added to permeabilized cells[3].
Immunofluorescence[3]
| Cell Line | chick lens cells, Swiss 3T3 fibroblasts, chicken embryo fibroblasts |
|---|---|
| Concentration | 300 μM |
| Incubation Time | 10 min, 30 min; 30 min incubation followed by 3-60 min recovery |
| Result | Caused rapid deterioration of actin-containing stress fibers and associated myosin, vinculin, and talin in focal contact sites within 10-30 min. Reorganized actin into short cytoplasmic bundles and lamellipodial protrusions. Retained actin, vinculin, and N-cadherin associated with cell-cell adherens junctions, with only minor increases in diffuse cytoplasmic N-cadherin staining. Reversed these effects upon removal: stress fibers reassembled within 3-10 min, with actin labeling augmented near adhesion sites, and the subcellular distribution of actin, myosin, vinculin, talin, and N-cadherin was restored within 60 min. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
