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H-89 . 2HCl

Protein kinase inhibitor
 
BML-EI196-0005 5 mg 95.00 USD
 
BML-EI196-0025 25 mg 397.00 USD
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Replaces Prod. #: ALX-270-017

Cell permeable potent and selective inhibitor of cAMP- and cGMP-dependent protein kinases (PKA, Ki=48nM, and PKG) and protein kinase Cµ (PKCµ). In contrast, most other protein kinase C (PKC) isotypes are much more weakly inhibited. Also inhibits Ca2+/calmodulin-dependent protein kinase II, casein kinase I and myosin light chain kinase. Induces apoptosis. Concentration range for cultured cells 30-100μM: osteoblastic cells, renal proximal tubule cells and Xenopus oocytes. 

Product Specification

Alternative Name:N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
 
Formula:C20H20BrN3O2S·2HCl
 
MW:519.3
 
CAS:127243-85-0
 
Purity:≥99% (HPLC)
 
Appearance:White to off-white solid.
 
MeltingPoint:141-143°C
 
Solubility:Soluble in DMSO (25mg/ml), methanol and 50% ethanol/water (20mg/ml).
 
Shipping:Ambient
 
Long Term Storage:+4°C
 
Use/Stability:Store, as supplied, at 0-4°C for up to 1 year. Store solutions at -20°C for up to 4 months in DMSO.
 
Technical Info/Product Notes:Replacement for ADI-HPK-105
 
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Product Literature References

Involvement of PI3K and PKA pathways in mouse tongue epithelial differentiation: J.K. Jung, et al.; Acta Histochem. 119, 92 (2017), Abstract;
Phosphoinositide 3-kinase γ ties chemoattractant- and adrenergic control of microglial motility: N. Schneble, et al.; Mol. Cell. Neurosci. 78, 1 (2016), Abstract;
Prostaglandin E2-stimulated prostanoid EP4 receptors induce prolonged de novo prostaglandin E2 synthesis through biphasic phosphorylation of extracellular signal-regulated kinases mediated by activation of protein kinase A in HCA-7 human colon cancer cells: H. Fujino, et al.; Eur. J. Pharmacol. 768, 149 (2015), Application(s): Cell culture , Abstract;
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells.: T. Bouschet et al.; J. Biol. Chem. 278, 4778 (2003), Abstract;
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.: R.A. Engh et al.; J. Biol. Chem. 271, 26157 (1996), Abstract;
Characterization of activators and inhibitors of protein kinase C mu.: F.J. Johannes et al.; Eur. J. Biochem. 227, 303 (1995), Abstract;
Parathyroid hormone and parathyroid hormone-related peptide activate the Na+/H+ exchanger NHE-1 isoform in osteoblastic cells (UMR-106) via a cAMP-dependent pathway.: A. Azarani et al.; J Biol Chem 270, 23166 (1995), Abstract;
Parathyroid hormone and parathyroid hormone-related peptide inhibit the apical Na+/H+ exchanger NHE-3 isoform in renal cells (OK) via a dual signaling cascade involving protein kinase A and C.: A. Azarani et al. ; J. Biol. Chem. 270, 20004 (1995), Abstract;
Protein kinase A inhibitors enhance radiation-induced apoptosis.: D. Findik et al.; J. Cell Biochem. 57, 12 (1995), Abstract;
Mechanism of lipopolysaccharide-triggered junB activation in a mouse macrophage-like cell line (J774).: M. Fujihara et al.; J. Biol. Chem. 268, 14898 (1993), Abstract;
Role of protein kinase A in LPS-induced activation of NF-kappa B proteins of a mouse macrophage-like cell line, J774.: M. Muroi & T. Suzuki; Cell Signal. 5, 289 (1993), Abstract;
A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells.: C.C. Geilen et al.; FEBS Lett. 309, 381 (1992), Abstract;
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 PC12: T. Chijiwa et al.; J. Biol. Chem. 265, 5267 (1990), Abstract;
Polyamines differentially inhibit cyclic AMP-dependent protein kinase-mediated phosphorylation in the brain of the tobacco hornworm, Manduca sexta.: W.L. Combest et al.; J. Neurochem. 51, 1581 (1988), Abstract;

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