H 89 2HCl
Catalog No.: GC10074Purity:>98.00%Synonyms: 5Isoquinolinesulfonamide, Protein Kinase Inhibitor H89
H 89 2HCl is a potent and selective cAMP-dependent protein kinase A (PKA) inhibitor with an IC50 value of 48nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130964-39-5
10mM (in 1mL DMSO)In Stock
$33.00
1
5mgIn Stock
$29.00
1
10mgIn Stock
$44.00
1
25mgIn Stock
$89.00
1
50mgIn Stock
$167.00
1
100mgIn Stock
$299.00
1
200mgIn Stock
$426.00
1
500mgIn Stock
$654.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $33.00 | In Stock | 1 | |
| 5mg | $29.00 | In Stock | 1 | |
| 10mg | $44.00 | In Stock | 1 | |
| 25mg | $89.00 | In Stock | 1 | |
| 50mg | $167.00 | In Stock | 1 | |
| 100mg | $299.00 | In Stock | 1 | |
| 200mg | $426.00 | In Stock | 1 | |
| 500mg | $654.00 | In Stock | 1 |
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Citations
3 publicationsPublications from researchers using this productDescription
H 89 2HCl is a potent and selective cAMP-dependent protein kinase A (PKA) inhibitor with an IC50 value of 48nM[1]. H 89 2HCl inhibits Rho kinase (ROCK) and PKA, thereby regulating the protrusions of contracting cells and influencing cell morphology[2]. H 89 2HCl has been widely used to block both endoplasmic reticulum (ER) export and hypo-osmotic-induced Golgi-to-ER transport[3].
In vitro, H 89 2HCl treatment for 72 hours significantly inhibited the proliferation of OVCAR-8, HL60, and HCT-116 cells, with IC50 values of 10.5µM, 11.4µM, and 15.7µM, respectively[4]. Treatment with 10μM H 89 2HCl for 24 hours induced autophagy in NG108-15 cells, accompanied by an increase in LC3-II levels and a decrease in mTOR activity[5]. Treatment with 6μM H 89 2HCl for 24 hours significantly increased the survival rate of human embryonic stem cells (hESCs) isolated after cryopreservation[6].
In vivo, H 89 2HCl treatment via intraperitoneal injection at a dose of 20mg/kg, three times a week for 7 days, alleviated airway inflammation in the asthma mouse model, reduced the number of mast cells and mucus production[7]. Oral administration of H 89 2HCl at a dose of 5mg/kg daily for 5 days alleviated dextran sulfate sodium (DSS) induced-colitis and promoted the clearance of Candida albicans in the intestinal tract of mice[8].
References:
[1] Chijiwa T, Mishima A, Hagiwara M, 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]. Journal of Biological Chemistry, 1990, 265(9): 5267-5272.
[2] Leemhuis J, Boutillier S, Schmidt G, et al. The protein kinase A inhibitor H89 acts on cell morphology by inhibiting Rho kinase[J]. The Journal of pharmacology and experimental therapeutics, 2002, 300(3): 1000-1007.
[3] Lee T H, Linstedt A D. Potential role for protein kinases in regulation of bidirectional endoplasmic reticulum-to-Golgi transport revealed by protein kinase inhibitor H89[J]. Molecular biology of the cell, 2000, 11(8): 2577-2590.
[4] Liu T, Zhan W, Wang Y, et al. Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors[J]. European journal of medicinal chemistry, 2014, 73: 167-176.
[5] Inoue H, Hase K, Segawa A, et al. H89 (N-[2-p-bromocinnamylamino-ethyl]-5-isoquinolinesulphonamide) induces autophagy independently of protein kinase A inhibition[J]. European journal of pharmacology, 2013, 714(1-3): 170-177.
[6] Zhang L, Xu Y, Xu J, et al. Protein kinase A inhibitor, H89, significantly enhances survival rate of dissociated human embryonic stem cells following cryopreservation[J]. Cell Proliferation, 2016, 49(5): 589-598.
[7] Reber L L, Daubeuf F, Nemska S, et al. The AGC kinase inhibitor H89 attenuates airway inflammation in mouse models of asthma[J]. PloS one, 2012, 7(11): e49512.
[8] Dumortier C, Charlet R, Bettaieb A, et al. H89 treatment reduces intestinal inflammation and Candida albicans overgrowth in mice[J]. Microorganisms, 2020, 8(12): 2039.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
OVCAR-8 cells |
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Preparation Method |
OVCAR-8 cells were cultivated in RPIM 1640 medium supplemented with 5% heat-inactivated fetal bovine serum (FBS), 1% penicillin-streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in a 96-well plate at a density of 4×103 cells/well for 24h, with three replicates for each treatment. Cells were incubated with H 89 2HCl (0, 1, 10, 50, and 100µM) for 72h, The cell viability was detected. |
|
Reaction Conditions |
0, 1, 10, 50, and 100µM; 72h |
|
Applications |
H 89 2HCl treatment inhibited the cell viability of OVCAR-8 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Female C57BL/6 mice |
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Preparation Method |
Female C57BL/6 mice (4-month-old; 18-22g) were maintained in a controlled environment at 22±1°C and 60% relative humidity under a 12h light/dark cycle, and were fed ad libitum. Mice were given 107 live C. albicans yeast cells in 300µl PBS by oral gavage on day 1. All mice were given DSS at a concentration of 1.5% (36-50kDa) in drinking water in order to induce colitis. DSS was given to mice for 14 days. For H 89 2HCl treatment, mice received 5mg/kg in 200µl PBS daily for 5 days by oral gavage. The mice were then sacrificed on Day 14 by cervical dislocation and the colon was collected to determine the fungal load and to carry out PCR and histological examination. |
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Dosage form |
5mg/kg/day; 5 days; p.o. |
|
Applications |
H 89 2HCl treatment significantly reduced inflammatory parameters in DSS-induced colitis and promoted the clearance of Candida albicans in the intestinal tract of mice. |
References: [1] Liu T, Zhan W, Wang Y, et al. Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors[J]. European journal of medicinal chemistry, 2014, 73: 167-176. [2] Dumortier C, Charlet R, Bettaieb A, et al. H89 treatment reduces intestinal inflammation and Candida albicans overgrowth in mice[J]. Microorganisms, 2020, 8(12): 2039. | |
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
130964-39-5
Synonyms
5Isoquinolinesulfonamide, Protein Kinase Inhibitor H89
Chemical Name
(E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride
SMILES
O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl
Molecular Formula
C20H20BrN3O2S.2HCl
Molecular Weight
519.28
Solubility
≥ 51.9mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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