H 89 2HCl

For research use only. Not for use in humans.

Catalog No.S1582

52 publications

H 89 2HCl Chemical Structure

Molecular Weight(MW): 519.28

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

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10mM (1mL in DMSO) USD 120 In stock
USD 90 In stock
USD 310 In stock
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Selleck's H 89 2HCl has been cited by 52 publications

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Biological Activity

Description H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.
Targets
PKA [1]
(Cell-free assay)		 S6K1 [2]
(Cell-free assay)
48 nM(Ki) 80 nM
In vitro

H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with Ki of 48 nM, exhibits 10-fold selectivity over PKG, exhibits >500-fold selectivity over PKC, MLCK, calmodulin kinase II and casein kinase I/II. Pretreatment of the cells with H-89 (30 μM) 1 h before the addition of forskolin markedly inhibits the forskolin-induced protein phosphorylation in a dose-dependent manner. [1] H89 also inhibits several other kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, respectively. [2][3] H89 also has activity at some cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR. [4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO  NWPSUWo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYixNEDPxE1? NF[3ZnMyKGh? MWfpcohq[mm2czC1MWhVKGmwZIXj[YQh[0GPUDDwdo9lfWO2aX;uJIRm[3KnYYPl MUGxNlU3QTB4OR?=
SK-N-MC M4XpNGZ2dmO2aX;uJGF{e2G7 NW\XbnVJOzBizszN MUeyOEBp NXHMUJVvTE2VTx?= NVPPWZdSemWmdXPld{B1cGViZH;3ck1z\We3bHH0bY9vKG:oIN8yNU1CWiCkeTDpd49xem:2ZYLlco9tKGK7IEWwKeKh MY[xNVcxPTR3NB?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-S6K1 / p-rpS6 / p-GSK3β; 

PubMed: 26939705     


KOPN-8 cells were treated with 10 μM H89 or vehicle (Con) for the indicated times. Total cell lysates were analyzed by Western Blot for anti-phospho-S6-Kinase 1 (p-S6K1(T389)), anti-total S6K1, anti-p-CREB(S133)/p-ATF-1, anti-p-ribosomal protein S6 (p-rpS䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

p-eNOS / T-eNOS / p-PKA; 

PubMed: 31035633     


Western blotting analysis of phosphorylated PKA (Thr197), total PKA, phosphorylated eNOS and total eNOS in control (Mock) and MAGI1 overexpressing (OE) HUVEC in the presence of absence of the PKA inhibitor H-89. PKA mediates MAGI1-induced eNOS phosphoryla䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뾠Ղ䐺痖暼瘿뾠Ղᾰƌ 뾠ՂÐ㺣痖뾠Ղ€𢡄뾤Ղ€䀷痗뾤Ղ౴뾤Ղ㵶痗뾤Ղ뺖᎒泌Item

p-GPIbβ / GPIbβ / p-BAD; 

PubMed: 29083324     


Washed platelets were incubated with indicated concentrations of H89 or vehicle at 22°C for 160 minutes. Western blot analysis for the levels of indicated proteins with different antibodies.

26939705 31035633 29083324
Immunofluorescence
myopodin; 

PubMed: 17923693     


In undifferentiated dimethyl sulfoxide (DMSO)-treated C2C12 myoblasts (control), myopodin is localized in the nucleus, as revealed by double-labeling deconvolution microscopy with DAPI. Pharmacological inhibition of CaMKII by KN62 partially reduces the nu䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ삨Ղ䐺痖暼瘿삨Ղᾰƌ 삨ՂÐ㺣痖삨Ղ€𢡄사Ղ€䀷痗사Ղ౴사Ղ㵶痗사Ղ뺖᎒泌Itemｾ᎒Count﫨呂샜Ղ猴፲사Ղ፲씢痗猸፲髸莤䥷堙᎒ｾ᎒�堞ﻮ᎒፲露𢡄堚Ԋ齃礤v�堞ﻮ᎒猢Wｾ᎒䨼Ą鹿齃殺獸W戀醙玛W戀ⶰ໯齃礤v 玚W玢Wⶰ໯﫰礌vtЉᔈැ鲬౴᥊疜犈፲Eo狜፲

iNOS / NFκB p65 ; 

PubMed: 30513637     


Immunofluorescence analysis of the effect of H89 on iNOS (green) and NF-κB p65 (red) level in α-MSH-treated HUVECs.

p-eNOS / eNOS ; 

PubMed: 30513637     


Immunofluorescence analysis of the effect of H89 on phospho-Ser1177-eNOS (red) and eNOS (green) expression in α-MSH-treated HUVECs. Cell nuclei were counterstained with DAPI (blue). Scale bars, 100 μm.

17923693 30513637
In vivo H89 causes distinct modifications of protein phosphorylation, with the most robust changes in phosphorylation are fructose-1,6-biphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), NSFL1 cofactor p47, all which have potentially regulatory connections to cAMP/PKA. [5] H-89 (0.5, 1, 5 mg/kg) significantly attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice.[6]

Protocol

Kinase Assay:[1]
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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 Research: [1]
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  • Cell lines: PC12D
  • Concentrations: ~30 μM
  • Incubation Time: 1 h
  • Method: Levels of intracellular cAMP are determined. After 48 h in culture, PC12D 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.
    (Only for Reference)
Animal Research:[5] [6]
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  • Animal Models: rat; mice
  • Formulation: Dissolved in 100% DMSO, diluted 1:20 in 0.9% sterile saline (Rat); 1% DMSO (Mice)
  • Dosages: 20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice)
  • Administration: s.c. (Rat); i.p. (Mice)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 104 mg/mL (200.27 mM)
Water 6 mg/mL (11.55 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 519.28
Formula

C20H20BrN3O2S.2HCl
CAS No. 130964-39-5
Storage powder
in solvent
Synonyms N/A
Smiles Cl.Cl.BrC1=CC=C(/C=C/CNCCN[S](=O)(=O)C2=CC=CC3=C2C=CN=C3)C=C1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID