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H 89 2HCl Potent PKA inhibitor

Catalog No.B2190
Size Price Stock Qty
10mM (in 1mL DMSO)
$65.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$63.00
In stock
50mg
$217.00
In stock
200mg
$616.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
2. Matos, Steven Cordeiro, et al. "Peripheral Neuropathy Induces HCN Channel Dysfunction in Pyramidal Neurons of the Medial Prefrontal Cortex." The Journal of Neuroscience 35.38 (2015): 13244-13256. PMID:26400952

Quality Control

Chemical structure

H 89 2HCl

Related Biological Data

SGX-523

Related Biological Data

SGX-523

Biological Activity

Description H 89 2HCl is a potent inhibitor of PKA with a Ki value of 48 nM.
Targets PKA S6K1        
IC50 48 nM(Ki) 80 nM        

Protocol

Kinase experiment [1]:

PKA enzyme activity

cAMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HC1 (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cAMP or absence of cAMP, 3.3-20 μM [γ-32P]ATP (4 × 105 cpm), 0.5 μg of the enzyme, 100 μg of histone H2B, and each compound, as indicated.

Cell experiment [1]:

Cell lines

PC12D cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

30 μM for 1h

Applications

H-89 (30 μM) significantly inhibited cAMP-dependent histone IIh phosphorylation activity and suppressed Forskolin-induced neurite outgrowth in PC12D cells.

Animal experiment [2]:

Animal models

Rats model

Dosage form

20 or 200 mg/kg; s.c. twice daily for 2 days;

Applications

H89 caused distinct modifications of protein phosphorylation, with the most robust changes in phosphorylation were heterogeneous nuclear ribonucleoprotein (hnRNP), fructose-1,6-biphosphatase, NSFL1 cofactor p47, all which had potentially regulatory connections to cAMP/PKA.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1Chijiwa, T., Mishima, A., Hagiwara, M., Sano, M., Hayashi, K., Inoue, T., Naito, K., Toshioka, T. and Hidaka, H. (1990) 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. 265, 5267-5272

2Davis, M. A., Hinerfeld, D., Joseph, S., Hui, Y. H., Huang, N. H., Leszyk, J., Rutherford-Bethard, J. and Tam, S. W. (2006) Proteomic analysis of rat liver phosphoproteins after treatment with protein kinase inhibitor H89 (N-(2-[p-bromocinnamylamino-]ethyl)-5-isoquinolinesulfonamide). J Pharmacol Exp Ther. 318, 589-595

H 89 2HCl Dilution Calculator

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Chemical Properties

Cas No. 130964-39-5 SDF Download SDF
Synonyms N/A
Chemical Name (E)-N-(2-((3-(4-bromophenyl)allyl)amino)ethyl)isoquinoline-5-sulfonamide dihydrochloride
Canonical SMILES O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.Cl.Cl
Formula C20H20BrN3O2S.2HCl M.Wt 519.28
Solubility >51.9mg/ml in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

H 89 2HCl is a potent PKA inhibitor. In a cell-free assay, the Ki of H 89 is 48 nM, 10-fold selective for PKA than PKG and 500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II [1].

In vitro:In PC12D cells, pretreatment with H-89 dose-dependently inhibited the forskolin-induced protein phosphorylation, with no influence in intracellular cyclic AMP levels. In PC12D cells, H-89 significantly inhibited the forskolin-induced neurite outgrowth. In PC12D cells, pretreatment with H-89 (30 μM) strikingly inhibited cAMP-dependent histone IIb phosphorylation activity in cell lysates while showed no effects on other protein phosphorylation activity such as cGMP-dependent histone IIb phosphorylation activity [1]. H 89 was a potent and selective PKA inhibitor with Ki of 48 nM in a cell-free assay [2]. H89 also inhibited S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM, respectively [2]. In the hypotonic medium, 50 μM H89, a concentration commonly used to inhibit PKA, prevented the redistribution response. In normal medium, H89 (50 Μm) induced the redistribution of ERGIC 53 to the ER by 20 min [3].

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]. Lochner A, Moolman J A. The many faces of H89: a review[J]. Cardiovascular drug reviews, 2006, 24(3‐4): 261-274.

[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

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