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Protein kinase inhibitor
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.
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Product Details
| Alternative Name |
N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl |
|---|---|
| Appearance |
White to off-white solid. |
| CAS |
127243-85-0 |
| Couple Target |
CaM kinase, Casein kinase, MLCK, PKA, PKD, PKG |
| Couple Type |
Inhibitor |
| Formula |
C20H20BrN3O2S·2HCl |
| MW |
519.3 |
| MeltingPoint |
141-143°C |
| Purity |
≥99% (HPLC) |
| Solubility |
Soluble in DMSO (25mg/ml), methanol and 50% ethanol/water (20mg/ml). |
| Technical Info / Product Notes |
Replacement for ADI-HPK-105 |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Store, as supplied, at 0-4°C for up to 1 year. Store solutions at -20°C for up to 4 months in DMSO. |
|---|---|
| Long Term Storage |
+4°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- 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
- Mislocalization of protein kinase A drives pathology in Cushing’s syndrome: Omar, M. H., Byrne, D. P., et al.; Cell Rep. 40, 111073 (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
- Inhibitory Effect and Mechanism of Arctium lappa Extract on NLRP3 Inflammasome Activation: Kim, Y. K., Koppula, S., et al.; Evid. Based Complement. Alternat. Med. 2018, 6346734 (2018), Abstract
- 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
- Dysregulation of hepatic cAMP levels via altered Pde4b expression plays a critical role in alcohol-induced steatosis: Avila, D. V., Barker, D. F., et al.; J. Pathol. 240, 96 (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
- Cystic fibrosis transmembrane conductance regulator activation by roflumilast contributes to therapeutic benefit in chronic bronchitis: Lambert, J. A., Raju, S. V., et al.; Am. J. Respir. Cell Mol. Biol. 50, 549 (2014), Abstract
- Phosphorylation of serine 4,642 in the C-terminus of plectin by MNK2 and PKA modulates its interaction with intermediate filaments: Bouameur, J. E., Schneider, Y., et al.; J. Cell Sci. 126, 4195 (2013), Abstract
- Decrease in the density of t-tubular L-type Ca2+ channel currents in failing ventricular myocytes: Horiuchi-Hirose, M., Kashihara, T., et al.; Am. J. Physiol. Heart Circ. Physiol. 300, H978 (2011), Abstract
- PPARgamma agonists inhibit TGF-beta-PKA signaling in glomerulosclerosis: Zou, R., Xu, G., et al.; Acta Pharmacol. Sin. 31, 43 (2010), 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
- 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
- Characterization of activators and inhibitors of protein kinase C mu.: F.J. Johannes et al.; Eur. J. Biochem. 227, 303 (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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