H-89

Name: H-89
Brand: MedChemExpress
SKU: HY-15979
Rating: 5.0 (179 reviews)

Cat. No.: HY-15979 Purity: 99.96%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 127243-85-0

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 179 publication(s) in Google Scholar

Other Forms of H-89:

H-89 dihydrochloride In-stock

179 Publications Citing Use of MCE H-89

Cell Proliferation/Viability Assay

RT-PCR

: H-89 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Feb;20(2):175-188. [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 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2023 Apr 2;19(7):2006-2019.; H-89 dihydrochloride (H-89; 10 μM; 2 h) blocks the epinephrine-induced phosphorylation of CREB1 in MC38 and HT-29 cells.

: H-89 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 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 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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PKA PKAR PKACα

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

IC50: 48 nM (protein kinase A)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	15.7 μM Compound: H-89	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24389511]
HCT-116	IC₅₀	15.7 μM Compound: H-89	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24508830]
HL-60	IC₅₀	11.4 μM Compound: H-89	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 24389511]
OVCAR-8	IC₅₀	10.5 μM Compound: H-89	Antiproliferative activity against human OVCAR8 cells after 72 hrs by MTT assay Antiproliferative activity against human OVCAR8 cells after 72 hrs by MTT assay	[PMID: 24389511]
OVCAR-8	IC₅₀	10.5 μM Compound: H-89	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24508830]
PC-3M	GI₅₀	18 μM Compound: H-89	Inhibition of PC3M cells by SRB assay after 96 hrs Inhibition of PC3M cells by SRB assay after 96 hrs	[PMID: 17451235]
PC-3M	IC₅₀	18 μM Compound: H-89	Growth inhibition of human PC3M cells by SRB assay Growth inhibition of human PC3M cells by SRB assay	[PMID: 18345609]
Sf9	IC₅₀	120 nM Compound: H89	Inhibition of His-tagged human MSK1 expressed in Sf9 cells Inhibition of His-tagged human MSK1 expressed in Sf9 cells	[PMID: 10998351]
Sf9	IC₅₀	2.6 μM Compound: H89	Inhibition of human PKBalpha expressed in SF9 cells Inhibition of human PKBalpha expressed in SF9 cells	[PMID: 10998351]
Sf9	IC₅₀	270 nM Compound: H89	Inhibition of rat ROCK2 expressed in Sf9 cells Inhibition of rat ROCK2 expressed in Sf9 cells	[PMID: 10998351]
U-87MG ATCC	IC₅₀	15 μM Compound: H-89	Growth inhibition of human U87MG cells by SRB assay Growth inhibition of human U87MG cells by SRB assay	[PMID: 18345609]
U-87MG ATCC	IC₅₀	15 μM Compound: H-89	Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay Antiproliferative activity against human U87MG cells after 96 hrs by SRB assay	[PMID: 20151677]

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 Ca³²-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.

분자량

446.36

화학식

C₂₀H₂₀BrN₃O₂S

CAS No.

127243-85-0

Appearance

Solid

Color

Off-white to light brown

SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (224.03 mM; Need ultrasonic; 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	2.2403 mL	11.2017 mL	22.4034 mL
5 mM	0.4481 mL	2.2403 mL	4.4807 mL
10 mM	0.2240 mL	1.1202 mL	2.2403 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.60 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.

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).

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.

순도&문서

Purity: 99.96%

Select Batch:

Data Sheet (278 KB) SDS (396 KB)

COA (245 KB) HNMR (235 KB) LCMS (141 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 pentoxifylline 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]

Kinase Assay ^[1]	Kinase activities are assayed at 30°C for 2-5 min by measuring the transfer of ³²P from [γ-³²P]ATP to substrates. The reaction is terminated by adding 1 mL of 20% trichloroacetic acid, following the addition of 100 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 rpm for 10 min, the pellet is resuspended in 5% trichloroacetic acid solution, the final pellet is dissolved in 1 mL of 1 N NaOH and the radioactivity is measured in a liquid scintillation counter. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[1]	Male albino mice weighing 20-25 g are obtained. Pentoxifylline (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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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 pentoxifylline 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

DMSO	1 mM	2.2403 mL	11.2017 mL	22.4034 mL	56.0086 mL
	5 mM	0.4481 mL	2.2403 mL	4.4807 mL	11.2017 mL
	10 mM	0.2240 mL	1.1202 mL	2.2403 mL	5.6009 mL
	15 mM	0.1494 mL	0.7468 mL	1.4936 mL	3.7339 mL
	20 mM	0.1120 mL	0.5601 mL	1.1202 mL	2.8004 mL
	25 mM	0.0896 mL	0.4481 mL	0.8961 mL	2.2403 mL
	30 mM	0.0747 mL	0.3734 mL	0.7468 mL	1.8670 mL
	40 mM	0.0560 mL	0.2800 mL	0.5601 mL	1.4002 mL
	50 mM	0.0448 mL	0.2240 mL	0.4481 mL	1.1202 mL
	60 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9335 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.7001 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5601 mL

H-89 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H-89127243-85-0H89H 89PKAAutophagyProtein kinase AInhibitorinhibitorinhibit

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H-89

고객리뷰

Other Forms of H-89:

H-89 Related Antibodies

179 Publications Citing Use of MCE H-89

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKA Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

H-89 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

H-89 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report