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H 89 2HCl

Name: H 89 2HCl
Brand: Selleck Chemicals
SKU: S1582
Rating: 5 (135 reviews)

Catalog No.S1582

For research use only.

H 89 2HCl is a potent PKA inhibitor with K_i 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. H 89 2HCl induces autophagy.

CAS No. 130964-39-5

Selleck's H 89 2HCl has been cited by 135 publications

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Biological Activity

Description

Targets

PKA ^[1] (Cell-free assay)	S6K1 ^[2] (Cell-free assay)	PKG ^[1] (Cell-free assay)
48 nM(Ki)	80 nM	0.48 μM(Ki)

In vitro

H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with K_i 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	NYPVcG43T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MojwNVAh\|ryP	MnXwNUBp		NX\sV3EycW6qaXLpeJMhPS2KVDDpcoR2[2WmIHPBUXAheHKxZIXjeIlwdiCmZXPy[YF{\Q>?	MoqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJ3NkmwOlkoRjF{NU[5NFY6RC:jPh?=
SK-N-MC	M{TJPGZ2dmO2aX;uJGF{e2G7	MUCzNEDPxE1?	NYHyNVFUOjRiaB?=	MYrEUXNQ	MWLy[YR2[2W\|IITo[UBld3ewLYLl[5Vt[XSrb36gc4Yh\|rJzLVHSJIJ6KGm\|b4Dyc5RmemWwb3ygZpkhPTBnwrC=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTdyNUS1OEc,OTF5MEW0OVQ9N2F-
Sf9	MkT4SpVv[3Srb36gZZN{[Xl?				NGDhdWdKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgbJVu[W5iTWPLNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy\|LDDJR\|UxKD1iMD6xNkDPxE1w	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODl7OEO1NUc,OTB7OUizOVE9N2F-
Sf9	M12xfGZ2dmO2aX;uJIF{e2G7				M13VWmlvcGmkaYTpc44hd2ZicnH0JHJQS0t{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUCgQUAxNjJ5IN88UU4>	NG\XXGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMEm5PFM2OSd-MUC5PVg{PTF:L3G+
SF9	NWW2R\|Z3TnWwY4Tpc44h[XO\|YYm=				MmXWTY5pcWKrdHnvckBw\iCqdX3hckBRU0KjbIDoZUBmgHC{ZYPz[YQhcW5iU1[5JINmdGy\|LDDJR\|UxKD1iMj62JO69VS5?	Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUizOVEoRjFyOUm4N\|UyRC:jPh?=
OVCAR8	NVnkT4I5S3m2b4TvfIlkcXS7IHHzd4F6		Mm\iO\|IhcHK\|		Mn2xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ6IHPlcIx{KGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzMD61JO69VS5?	MlL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEi4N\|AoRjJ2NUC4PFMxRC:jPh?=
OVCAR8	NFPONVNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NWTWN3E5PzJiaILz		NYnDR2xxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFExNjVizszNMi=>	NYLsWpZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPFk2OTFpPkK0N\|g6PTFzPD;hQi=>
HL60	MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NF7yeGo4OiCqcoO=		Mom2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKTE[wJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzMT60JO69VS5?	NFrNU3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO4PVUyOSd-MkSzPFk2OTF:L3G+
PC3M	MWTGeY5kfGmxbjDhd5NigQ>?				MlnlTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iUFOzUUBk\WyuczDifUBGVEmVQTygTWM2OCB;IEG1JO69VS5?	M2HjR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{S1OlA6Lz5zOEO0OVYxQTxxYU6=
U87MG	MnfuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?				NIP2Z\|RIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBWQDePRzDj[YxteyCkeTDTVmIh[XO\|YYmsJGlEPTBiPTCxOUDPxE1w	Mk[zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh\|NEW2NFkoRjF6M{S1OlA6RC:jPh?=
U87MG	NH;zd3VCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MmPoPVYhcHK\|		MknFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCXOEfNS{Bk\WyuczDh[pRmeiB7NjDodpMh[nliU2LCJIF{e2G7LDDJR\|UxKD1iMUWg{txONg>?	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF3MU[3O{c,OjBzNUG2O\|c9N2F-
HCT116	Mmi3R5l1d3SxeHnjbZR6KGG\|c3H5		NHzG[4w4OiCqcoO=		NYq4SGtxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy\|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCxOU44KM7:TT6=	NYGxcWJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFg5OzBpPkK0OVA5QDNyPD;hQi=>
HCT116	M{T0VmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		M3u1UVczKGi{cx?=		M1PsSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCxOU44KM7:TT6=	M1;2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{i5OVEyLz5{NEO4PVUyOTxxYU6=
PC3M	NWLkN5JJTnWwY4Tpc44h[XO\|YYm=		MWm5OkBpenN?		NYDu[lJDUW6qaXLpeIlwdiCxZjDQR\|NOKGOnbHzzJIJ6KFOUQjDhd5NigSCjZoTldkA6PiCqcoOsJGdKPTBiPTCxPEDPxE1w	M{PrTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEWxNlM2Lz5zN{S1NVI{PTxxYU6=
PC3M	M2LMd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7				MUTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDQR\|NOKGOnbHzzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDF6IN88UU4>	NVXETpFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOFU3ODlpPkG4N\|Q2PjB7PD;hQi=>
LS174T	M2\XeWZ2dmO2aX;uJIF{e2G7	NVTHWIlROjBidV2=	M{\jc\|YhcHK\|		M{GzXGlvcGmkaYTpc44hd2ZiUFfFNk1{fGmvdXzheIVlKFSFRj;MSWYhfHKjboPhZ5RqfmG2aX;uJIlvKGi3bXHuJGxUOTd2VDDj[YxteyCjdDCyNEB2VSCvZXHzeZJm\CCjZoTldkA3KGi{czDifUBlfWGuIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=>	NH3r[pc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ezOlA3Oyd-Mke3N\|YxPjN:L3G+

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p-S6K1 / p-rpS6 / p-GSK3β ; p-eNOS / T-eNOS / p-PKA ; p-GPIbβ / GPIbβ / p-BAD	26939705 31035633 29083324
Immunofluorescence	myopodin ; iNOS / NFκB p65 ; p-eNOS / eNOS	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 (from reference)

Kinase Assay:^[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 Research: ^[1]	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.
Animal Research:^[5] ^[6]	Animal Models: rat; mice Dosages: 20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice) Administration: s.c. (Rat); i.p. (Mice)

References

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Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	519.28
Formula	C₂₀H₂₀BrN₃O₂S.2HCl
CAS No.	130964-39-5
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNCC=CC3=CC=C(C=C3)Br.Cl.Cl

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