Protein kinase inhibitor H-7

Name: Protein kinase inhibitor H-7
Brand: MedChemExpress
SKU: HY-131900
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Cat. No.: HY-131900 Pureté: 99.96%: Fiche technique
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Protein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with a K_i value of 6.0 μM for rabbit protein kinase C, a K_i value of 3.0 μM for rabbit cAMP-dependent protein kinase, and a K_i value of 5.8 μM for porcine cGMP-dependent protein kinase. Protein kinase inhibitor H-7 has no effect on Ca²⁺-calmodulin-dependent enzymes. Protein kinase inhibitor H-7 regulates the Actin cytoskeleton, inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid and reversible cytoskeletal reorganization. Protein kinase inhibitor H-7 serves as a research tool for elucidating the functions of protein kinase C-mediated signaling systems.

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Protein kinase inhibitor H-7 Chemical Structure

CAS No. : 84477-87-2

Size	Stock	Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtenir un devis
500 mg	Obtenir un devis

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Based on 1 publication(s) in Google Scholar

Other Forms of Protein kinase inhibitor H-7:

Protein kinase inhibitor H-7 dihydrochloride In-stock
Protein kinase inhibitor H-7 (Standard) Obtenir un devis

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform PKC:

Voir toutes les isoformes

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Voir tous les produits spécifiques à Isoform PKA:

Voir toutes les isoformes

PKA PKAR PKACα

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Description

IC₅₀ & Target^[1]

PKC

6 μM (Ki)

PKA

3 μM (Ki)

PKG

5.8 μM (Ki)

In Vitro

The protein kinase inhibitor H-7 potently and directly inhibits rabbit brain protein kinase C (K_i = 6.0 μM) and rabbit skeletal muscle cAMP-dependent protein kinase (K_i = 3.0 μM), but exhibits weak activity against other purified protein kinases and ATPases from multiple species and tissues^[1].
Protein kinase inhibitor H-7 (10-50 μM; 2 min preincubation) dose-dependently inhibits protein kinase C-mediated phosphorylation of the 40K protein in intact washed rabbit platelets, but does not inhibit Ca²⁺-calmodulin-mediated phosphorylation of the 20K protein in the same cellular system even at a concentration of 50 μM^[2].
The protein kinase inhibitor H-7 (100-300 μM) enhances lamellipodial protrusive activity and reduces cell polarity in Swiss 3T3 fibroblasts and SVT2 transformed fibroblasts, which is manifested by a significant increase in dispersion value and a significant decrease in elongation value^[3].
The protein kinase inhibitor H-7 (300 μM; 10-30 min) disrupts stress fibers and focal adhesion-related proteins (myosin, vinculin, talin) in chicken lens cells, while preserving intercellular adherens junctions, and these cytoskeletal changes are fully reversible after removal of H-7^[3].
When used as a pretreatment, the protein kinase inhibitor H-7 (300 μM; 10-15 min pretreatment, or added during permeabilization/contraction) potently inhibits ATP-induced contraction in Saponin (HY-100597)-permeabilized Swiss 3T3 fibroblasts, chicken lens cells and chicken embryo fibroblasts, but only weakly inhibits contraction when added to permeabilized cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Masse moléculaire

291.38

Formule

C₁₄H₁₇N₃O₂S

CAS No.

84477-87-2

Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(N3C(C)CNCC3)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (343.19 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4319 mL	17.1597 mL	34.3194 mL
5 mM	0.6864 mL	3.4319 mL	6.8639 mL
10 mM	0.3432 mL	1.7160 mL	3.4319 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Pureté et documentation

Purity: 99.96%

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Fiche technique (277 KB) SDS (252 KB)

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Références

[1]. Hidaka H, et al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41. [Content Brief]

[2]. Kawamoto S, et al. 1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets. Biochem Biophys Res Commun. 1984;125(1):258-264.

[3]. Volberg T, et al. Effect of protein kinase inhibitor H-7 on the contractility, integrity, and membrane anchorage of the microfilament system. Cell Motil Cytoskeleton. 1994;29(4):321-338.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4319 mL	17.1597 mL	34.3194 mL	85.7986 mL
	5 mM	0.6864 mL	3.4319 mL	6.8639 mL	17.1597 mL
	10 mM	0.3432 mL	1.7160 mL	3.4319 mL	8.5799 mL
	15 mM	0.2288 mL	1.1440 mL	2.2880 mL	5.7199 mL
	20 mM	0.1716 mL	0.8580 mL	1.7160 mL	4.2899 mL
	25 mM	0.1373 mL	0.6864 mL	1.3728 mL	3.4319 mL
	30 mM	0.1144 mL	0.5720 mL	1.1440 mL	2.8600 mL
	40 mM	0.0858 mL	0.4290 mL	0.8580 mL	2.1450 mL
	50 mM	0.0686 mL	0.3432 mL	0.6864 mL	1.7160 mL
	60 mM	0.0572 mL	0.2860 mL	0.5720 mL	1.4300 mL
	80 mM	0.0429 mL	0.2145 mL	0.4290 mL	1.0725 mL
	100 mM	0.0343 mL	0.1716 mL	0.3432 mL	0.8580 mL