H 89 2HCl

CAS No. 130964-39-5

H 89 2HCl( 5-Isoquinolinesulfonamide | Protein Kinase Inhibitor H-89 )

Catalog No. M11238 CAS No. 130964-39-5

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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100MG 327 In Stock
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Biological Information

  • Product Name
    H 89 2HCl
  • Note
    Research use only, not for human use.
  • Brief Description
    H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG.
  • Description
    H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.(In Vitro):H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca2+ uptake by the SR and affectes the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres.(In Vivo):H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.
  • In Vitro
    H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca2+ uptake by the SR and affectes the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres.
  • In Vivo
    H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.
  • Synonyms
    5-Isoquinolinesulfonamide | Protein Kinase Inhibitor H-89
  • Pathway
    Apoptosis
  • Target
    PKA
  • Recptor
    PKA| S6K1
  • Research Area
    Other Indications
  • Indication
    ——

Chemical Information

  • CAS Number
    130964-39-5
  • Formula Weight
    519.28
  • Molecular Formula
    C20H20BrN3O2S.2HCl
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:104 mg/mL (200.27 mM); Ethanol:<1 mg/mL (<1 mM); Water:6 mg/mL (11.55 mM)
  • SMILES
    C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Chijiwa T, et al. J Biol Chem., 1990, 265(9), 5267-5272.
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