H 89 2HCl

Alias: H-89; H 89 HCl; H-89 Dihydrochloride; H89
Cat No.:V0243 Purity: ≥98%
H 89 2HCl is a highly selective inhibitor of protein kinase a (PKA).
H 89 2HCl Chemical Structure CAS No.: 130964-39-5
Product category: S6 kinase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of H 89 2HCl:

  • H-89 free base
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
H 89 2HCl has a 48 nM IC50 and is a weak inhibitor of PKG, PKC, and casein kinase, but it is a strong and selective inhibitor of protein kinase A (PKA).
Biological Activity I Assay Protocols (From Reference)
Targets
PKA (Ki = 48 nM); S6K1 (IC50 = 80 nM); PKG (Ki = 0.48 μM)
ln Vitro
orskolin-induced protein phosphorylation is markedly and dose-dependently inhibited by pretreating the cells with H-89 (30 M) 1 hour before the addition of forskolin. [1] Other kinases that are inhibited by H89 include S6K1, MSK1, PKA, ROCKII, PKB, and MAPKAP-K1b, with IC50 values of 80, 120, 135, 270, 2600, and 2800 nM, respectively. [2] [3] Several cellular receptors and ion channels, including Kv1.3 K+ channels, 1AR, and 2AR, are also active in response to H89.[4] Forskolin-induced protein phosphorylation is markedly and dose-dependently inhibited by pretreating the cells with H-89 (30 M) 1 hour before the addition of forskolin. [1] Other kinases that are inhibited by H89 include S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, with IC50 values of 80, 120, 135, 270, 2600, and 2800 nM, respectively. [2] [3] Several cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR., are also active in response to H89. [4]
ln Vivo
The protein phosphorylation of H89 is altered in a variety of ways, but fructose-1,6-bisphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), and NSFL1 cofactor p47 exhibit the strongest phosphorylation changes. These proteins may all have regulatory relationships with cAMP/PKA. [5]
Enzyme Assay
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 Assay
Levels of intracellular cAMP are determined. After 48 hours of culture, PC12D cells are grown for 1 hour in test medium containing 30 μM H-89 before being exposed to brand-new medium containing 10 μM forskolin and 30 μM H-89. 0.5 ml of 6% trichloroacetic acid is added while cells are scraped off with a rubber policeman and sonicated. 2 ml of petroleum ether is added, the mixture is mixed, and the solution is centrifuged at 3000 rpm for 10 minutes to extract the trichloroacetic acid. The residue sample solution is used for analysis after aspiration of the top layer.
Animal Protocol
rat; mice
20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice)
s.c. (Rat); i.p. (Mice)
References

[1]. J Biol Chem . 1990 Mar 25;265(9):5267-72.

[2]. Biochem J . 2000 Oct 1;351(Pt 1):95-105.

[3]. Cardiovasc Drug Rev . 2006 Fall-Winter;24(3-4):261-74.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H24BRCL2N3O3S
Molecular Weight
519.28
Elemental Analysis
C, 46.26; H, 4.27; Br, 15.39; Cl, 13.65; N, 8.09; O, 6.16; S, 6.17
CAS #
130964-39-5
Appearance
Solid powder
SMILES
C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl
InChi Key
GELOGQJVGPIKAM-WTVBWJGASA-N
InChi Code
InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;
Chemical Name
N-[2-[[(E)-3-(4-bromophenyl)prop-2-enyl]amino]ethyl]isoquinoline-5-sulfonamide;dihydrochloride
Synonyms
H-89; H 89 HCl; H-89 Dihydrochloride; H89
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~104 mg/mL (~200.3 mM)
Water: ~6 mg/mL (~11.6 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9257 mL 9.6287 mL 19.2574 mL
5 mM 0.3851 mL 1.9257 mL 3.8515 mL
10 mM 0.1926 mL 0.9629 mL 1.9257 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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