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 Details
Alternative Name: | N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl |
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Formula: | C20H20BrN3O2S·2HCl |
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MW: | 519.3 |
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CAS: | 127243-85-0 |
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Purity: | ≥99% (HPLC) |
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Appearance: | White to off-white solid. |
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MeltingPoint: | 141-143°C |
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Solubility: | Soluble in DMSO (25mg/ml), methanol and 50% ethanol/water (20mg/ml). |
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Shipping: | Ambient Temperature |
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Long Term Storage: | +4°C |
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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. |
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Technical Info/Product Notes: | Replacement for ADI-HPK-105 |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
PAX9 Is Involved in Periodontal Ligament Stem Cell-like Differentiation of Human-Induced Pluripotent Stem Cells by Regulating Extracellular Matrix: R. Sugiura, et al.; Biomedicines
10, 2366 (2022),
Abstract;
Effect of selective serotonin (5-HT)2B receptor agonist BW723C86 on epidermal growth factor/transforming growth factor-α receptor tyrosine kinase and ribosomal p70 S6 kinase activities in primary cultures of adult rat hepatocytes: K. Naito, et al.; Biol. Pharm. Bull.
42, 631 (2019),
Application(s): used w. adult rat liver hepatocytes,
Abstract;
Full Text
Sensory innervation in porous endplates by Netrin-1 from osteoclasts mediates PGE2-induced spinal hypersensitivity in mice: S. Ni, et al.; Nat. Commun.
11, 149 (2019),
Abstract;
Full Text
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;