H-89 dihydrochloride

Name: H-89 dihydrochloride
Brand: MedChemExpress
SKU: HY-15979A
Rating: 5.0 (125 reviews)

Cat. No.: HY-15979A Purity: 99.12%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.

For research use only. We do not sell to patients.

H-89 dihydrochloride Chemical Structure

CAS No. : 130964-39-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 74	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 74	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 43	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 67	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 259	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 440	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 125 publication(s) in Google Scholar

Other Forms of H-89 dihydrochloride:

H-89 Get quote

120 Publications Citing Use of MCE H-89 dihydrochloride

Proliferation Assay

RT-PCR

: H-89 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Jan 5. [Abstract]; H89 (5 μM; 6 h) reverses ISO (Isoprenaline hydrochloride)-triggered decreases in the mRNA levels of the IFNB1 gene, the expression of which has been induced by SeV infection, in THP1 cells.

: H-89 dihydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2023 Apr 2,19.; H-89 dihydrochloride (H-89; 10 μM; 2 h) blocks the epinephrine-induced phosphorylation of CREB1 in MC38 and HT-29 cells.

: H-89 dihydrochloride purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2018 Jul 24;10(7):1722-1744. [Abstract]; Expressions of p-eNOS (Ser1177) and total eNOS are measured in HUVECs treated with or without H₂O₂ and Hemin in the presence or absence of Akt inhibitor MK-2206, PKA inhibitor H-89 or AMPK inhibitor Compound C (CP-C).

: H-89 dihydrochloride purchased from MedChemExpress. Usage Cited in: Infect Immun. 2018 Dec 19;87(1). pii: e00508-1 [Abstract]; J774A.1 cells are pre-treated with 473 U0126 (10 μM), SB208530 (10 μM), SP600125 (10 μM), or H89 (50 μM), then infected with ΔeseH E. piscicida at the MOI of 10 for 3.5 h. Cell lysates were probed with anti-phospho-p65 (Ser276), anti-p65, and anti-β-actin antibodies.

: H-89 dihydrochloride purchased from MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]; The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.

IC₅₀ & Target

IC50: 48 nM (protein kinase A)

In Vitro

H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates^[1]. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca²⁺ uptake by the SR and affectes the Ca²⁺-sensitivity of the contractile apparatus in rat skinned fibres^[2].

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

In Vivo

H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold^[3].

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

Molecular Weight

519.28

Formula

C₂₀H₂₂BrCl₂N₃O₂S

CAS No.

130964-39-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (192.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (9.63 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9257 mL	9.6287 mL	19.2574 mL
5 mM	0.3851 mL	1.9257 mL	3.8515 mL
10 mM	0.1926 mL	0.9629 mL	1.9257 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Saline
Solubility: 5 mg/mL (9.63 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (5.30 mM); Clear solution
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (5.30 mM); Clear solution
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 7

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.55 mg/mL (1.06 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.34%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (247 KB) LCMS (119 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)

References

[1]. Chijiwa T, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol Chem. 1990 Mar 25;265(9):5267-72. [Content Brief]

[2]. Blazev R, et al. Effects of the PKA inhibitor H-89 on excitation-contraction coupling in skinned and intact skeletal muscle fibres. J Muscle Res Cell Motil. 2001;22(3):277-86. [Content Brief]

[3]. Hosseini-Zare MS, et al. Effects of BL-191 and H-89 on epileptogenic activity of bucladesine in pentylenetetrazol-treated mice. Eur J Pharmacol. 2011 Nov 30;670(2-3):464-70. [Content Brief]

Cell Assay ^[1]	After 48 h in culture, PCl2D cells are cultured in test medium containing 30 μM H-89 for 1 h and then exposed to fresh medium that contained both 10 μM forskolin and 30 μM H-89. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5 mL of 6% trichloroacetic acid. To extract trichloroacetic acid, 2 mL of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Male albino mice weighing 20-25 g are obtained. BL-191 (25, 50, 100 mg/kg), bucladesine (50, 100, 300 nM/mouse) and H-89 (0.05, 0.1, 0.2 mg/100 g) are administered intraperitoneally (i.p.) 30 min before intravenous (i.v.) infusion of PTZ. In combination groups, the first and second components are injected 45 and 30 min before PTZ infusion. In all groups, the respective control animalsreceive an appropriate volume of vehicle. For the i.v. infusion, the needle is inserted into the lateral tail vein, fixed to the tail vein by a narrow piece of adhesive tape, and the animal is allowed to move freely. PTZ solution is infused at a concentration rate of 1 mL/min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Chijiwa T, et al. Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells. J Biol Chem. 1990 Mar 25;265(9):5267-72. [Content Brief] [2]. Blazev R, et al. Effects of the PKA inhibitor H-89 on excitation-contraction coupling in skinned and intact skeletal muscle fibres. J Muscle Res Cell Motil. 2001;22(3):277-86. [Content Brief] [3]. Hosseini-Zare MS, et al. Effects of BL-191 and H-89 on epileptogenic activity of bucladesine in pentylenetetrazol-treated mice. Eur J Pharmacol. 2011 Nov 30;670(2-3):464-70. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	1.9257 mL	9.6287 mL	19.2574 mL	48.1436 mL
H₂O / DMSO	5 mM	0.3851 mL	1.9257 mL	3.8515 mL	9.6287 mL
DMSO	10 mM	0.1926 mL	0.9629 mL	1.9257 mL	4.8144 mL
	15 mM	0.1284 mL	0.6419 mL	1.2838 mL	3.2096 mL
	20 mM	0.0963 mL	0.4814 mL	0.9629 mL	2.4072 mL
	25 mM	0.0770 mL	0.3851 mL	0.7703 mL	1.9257 mL
	30 mM	0.0642 mL	0.3210 mL	0.6419 mL	1.6048 mL
	40 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2036 mL
	50 mM	0.0385 mL	0.1926 mL	0.3851 mL	0.9629 mL
	60 mM	0.0321 mL	0.1605 mL	0.3210 mL	0.8024 mL
	80 mM	0.0241 mL	0.1204 mL	0.2407 mL	0.6018 mL
	100 mM	0.0193 mL	0.0963 mL	0.1926 mL	0.4814 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.